Ep 2 136 209 A1

(19) &

(11) EP 2 136 209 A1

(12) EUROPEAN PATENT APPLICATION published in accordance with Art. 153(4) EPC

(43) Date of publication: (51) Int Cl.: 23.12.2009 Bulletin 2009/52 G01N 33/15 (2006.01) G01N 33/50 (2006.01)

(21) Application number: 08721397.1 (86) International application number: PCT/JP2008/053977 (22) Date of filing: 05.03.2008 (87) International publication number: WO 2008/111464 (18.09.2008 Gazette 2008/38)

(84) Designated Contracting States: • SAGANE, Koji AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Tsukuba-shi HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT Ibaraki 300-2635 (JP) RO SE SI SK TR • UESUGI, Mai Tsukuba-shi (30) Priority: 05.03.2007 US 904774 P Ibaraki 300-2635 (JP) 28.09.2007 US 960403 P • KADOWAKI, Tadashi Tsukuba-shi (71) Applicant: Eisai R&D Management Co., Ltd. Ibaraki 300-2635 (JP) Tokyo 112-8088 (JP) • YOSHIDA, Taku Tsukuba-shi (72) Inventors: Ibaraki 300-2635 (JP) • MIZUI, Yoshiharu Tsukuba-shi (74) Representative: Woods, Geoffrey Corlett Ibaraki 300-2635 (JP) J.A. Kemp & Co. • HATA, Naoko 14 South Square Tsukuba-shi Gray’s Inn Ibaraki 300-2635 (JP) London • IWATA, Masao WC1R 5JJ (GB) Tsukuba-shi Ibaraki 300-2635 (JP)

(54) METHOD FOR EXAMINATION OF ACTION OF ANTI-CANCER AGENT UTILIZING SPLICING DEFECT AS MEASURE

(57) An object of the present invention is to provide a method, a probe, a primer, an antibody, a reagent, and a kit for assaying an action of a pladienolide derivative to a living subject. According to the present invention, there is provided a method for assaying an action of the pladienolide derivative using splicing defect as an index. EP 2 136 209 A1

Printed by Jouve, 75001 PARIS (FR) EP 2 136 209 A1

Description

BACKGROUND OF THE INVENTION

5 Field of the Invention

[0001] The present invention relates to a method for assaying an action of an antitumor agent using splicing defect as an index, more particularly, a method for assaying an action of an antitumor agent using an increase in the expression level of pre-mRNA or abnormal protein as an index. 10 Background Art

[0002] Pladienolide derivatives are derivatives of natural pladienolide. Since pladienolide exhibits an excellent antitumor activity (Mizui et al., 2004, J. Antibiotics 577:188-196), search for a compound with higher antitumor activities has 15 been performed to find the pladienolide derivatives (WO2002/060890 and WO2003/099813).

SUMMARY OF THE INVENTION

[0003] The present inventors have found that pre-mRNA of a certain group of genes and abnormal proteins increase 20 when a pladienolide derivative is contacted with a sample obtained from living cells including cancerous cells, and peripheral blood (PBMC) and whole blood (PBC) of a subject. Without wishing to be bound by any theory, administration of the pladienolide derivative may cause an introduction of a mutation in pre-mRNA of a certain group of genes thereby inducing splicing defect. The present invention was made based on such findings. [0004] It is an object of the present invention to provide a method, a probe, a primer, an antibody, a reagent and a kit 25 for assaying an action of the pladienolide derivative on a living subject. [0005] According to the present invention, there are provided inventions (1) to (19) as follows. [0006] (1) A method for assaying an action of a compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a solvate of them to a mammal, which comprises detecting splicing defect caused by the compound represented by formula (I), the pharmaceutically acceptable salt thereof, or the solvate of them: 30 [0007]

wherein R3, R6, R7 and R21, the same or different, each represents

1) a hydroxyl group or an oxo group formed together with the carbon atom to which it is bound, provided that R6 is 50 limited to a hydroxyl group, 2) an optionally substituted C1-22 alkoxy group, 3) an optionally substituted unsaturated C2-22 alkoxy group, 4) an optionally substituted C7-22 aralkyloxy group, 5) an optionally substituted 5- to 14-membered heteroaralkyloxy group, 55 6) RCO-O- wherein R represents

a) a hydrogen atom, b) an optionally substituted C1-22 alkyl group,

2 EP 2 136 209 A1

c) an optionally substituted unsaturated C2-22 alkyl group, d) an optionally substituted C6-14 aryl group, e) an optionally substituted 5- to 14-membered heteroaryl group, f) an optionally substituted C7-22 aralkyl group, 5 g) an optionally substituted 5- to 14-membered heteroaralkyl group, h) an optionally substituted C1-22 alkoxy group, i) an optionally substituted unsaturated C2-22 alkoxy group, j) an optionally substituted C6-14 aryloxy group or k) an optionally substituted 5- to 14-membered heteroaryloxy group, 10 7) RS1 RS2RS3SiO- wherein RS1, RS2, and RS3, the same or different, each represents

a) a C1-6 alkyl group or b) a C6-14 aryl group, 15 8) a halogen atom, 9) RN1RN2N-RM- wherein RM represents

a) a single bond, 20 b) -CO-O-, c) -SO2-O-, d) -CS-O-or N3 N3 e) -CO-NR - wherein R represents a hydrogen atom or an optionally substituted C1-6 alkyl group, provided that each of the leftmost bond in b) to e)is bound to the nitrogen atom; and RN1 and RN2, the same or different 25 from each other and each represents

a) a hydrogen atom, b) an optionally substituted C1-22 alkyl group, c) an optionally substituted unsaturated C2-22 alkyl group, 30 d) an optionally substituted aliphatic C2-22 acyl group, e) an optionally substituted aromatic C7-15 acyl group, f) an optionally substituted C6-14 aryl group, g) an optionally substituted 5- to 14-membered heteroaryl group, h) an optionally substituted C7-22 aralkyl group, 35 i) an optionally substituted C1-22 alkylsulfonyl group, j) an optionally substituted C6-14 arylsulfonyl group, k) an optionally substituted 3- to 14-membered non-aromatic heterocyclic group formed by RN1 and RN2 together with the nitrogen atom to which RN1 and RN2 are bound, and the non-aromatic heterocyclic group optionally has substituent(s), 40 l) an optionally substituted 5- to 14-membered heteroaralkyl group, m) an optionally substituted C3-14 cycloalkyl group or n) an optionally substituted 3- to 14-membered non-aromatic heterocyclic group,

N4 N4 10) R SO2-O- wherein R represents 45

a) an optionally substituted C1-22 alkyl group, b) an optionally substituted C6-14 aryl group, c) an optionally substituted C1-22 alkoxy group, d) an optionally substituted unsaturated C2-22 alkoxy group, 50 e) an optionally substituted C6-14 aryloxy group, f) an optionally substituted 5- to 14-membered heteroaryloxy group, g) an optionally substituted C7-22 aralkyloxy group or h) an optionally substituted 5- to 14-membered heteroaralkyloxy group,

55 N5 N5 11) (R O)2PO-O- wherein R represents

a) an optionally substituted C1-22 alkyl group, b) an optionally substituted unsaturated C2-22 alkyl group,

3 EP 2 136 209 A1

c) an optionally substituted C6-14 aryl group, d) an optionally substituted 5- to 14-membered heteroaryl group, e) an optionally substituted C7-22 aralkyl group or f) an optionally substituted 5- to 14-membered heteroaralkyl group, 5 N1 N2 N1 N2 12) (R R N)2PO-O- wherein R and R have the same meanings as defined above or 13) (RN1RN2N)(RN5O)PO-O- wherein RN1, RN2 and RN5 have the same meanings as defined above, provided that a compound in which R3, R6, R7 and R21 are all hydroxyl groups, and a compound in which R3, R6 and R21 are all hydroxyl groups and R7 is an acetoxy group are excluded, 10 R16 represents a hydrogen atom or hydroxyl group. (2) The method according to (1), wherein the compound represented by formula (I) is selected from the group consisting of:

(8E,12E,14E)-7-(N-(2-(N’,N’-Dimethylamino)ethyl)-N-methylcarbamoyloxy)-3,6,16,21-tetrahydroxy- 15 6,10,12,16,20-pentamethyl18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-6,10,12,16,20-pentamethyl-7-((4-methylhomopiperazin-1-yl)carbonyl) oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-6,10,12,16,20-pentamethyl-7-((4-methyl piperazin-1-yl)carbonyl)oxy- 18,19-epoxytricosa-8,12,14-trien-11-olide; 20 (8E,12E,14E)-7-((4-Butylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl- 18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Ethylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl- 18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-6,10,12,16,20-pentamethyl-7-((4-propylpiperazin-1-yl)carbonyl)oxy- 25 18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Cyclohexylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-(Cyclopropylmethyl)piperazin-1-yl)carbonyl)oxy-3,6,16, 21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; 30 (8E,12E,14E)-3,6,16,21-Tetrahydroxy-6,10,12,16,20-pentamethyl-7-((4-propylhomopiperazin-1-yl)carbonyl) oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-(Cyclopropylmethyl)homopiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16, 20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Cyclopentylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentame- 35 thyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-7-((4-isopropylpiperazin-1-yl)carbonyl)oxy-6,10,12,16,20-pentamethyl- 18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-Tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; 40 (8E,12E,14E)-7-(N-(2-(N’,N’-Diethylamino)ethyl)-N-methylcarbamoyloxy)-3,6,16,21-tetrahydroxy- 6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-7-((4-isobutylhomopiperazin-1-yl)carbonyl)oxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Ethylhomopiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentame- 45 thyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Butylhomopiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,16,21-Trihydroxy-6-methoxy-6,10,12,16,20-pentamethyl-7-((4-methylpiperazin-1-yl)carbonyl) oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; 50 (8E,12E,14E)-3,16,21-Trihydroxy-6-methoxy-6,10,12,16,20-pentamethyl-7-((4-(piperidin-1-yl)piperidin-1-yl) carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,7,21-Tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-(2,2-Dimethylpropyl)homopiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy- 6,10,12,16,20-pentamethyl-1-8,19-epoxytricosa-8,12,14-trien-11-olide; and 55 (8E,12E,14E)-3,6,16-Trihydroxy-21-methoxy-6,10,12,16,20-pentamethyl-7-((4-methylpiperazin-1-yl)carbonyl) oxy-18,19-epoxytricosa-8,12,14-trien-11-olide.

[0008] (3) The method according to (1), wherein the detection of splicing defect comprises the steps of:

4 EP 2 136 209 A1

(a) measuring the expression level of pre-mRNA before and after administration of the compound represented by formula (I), the pharmaceutically acceptable salt thereof ,or the solvate of them to a mammal; (b) comparing, based on the expression level measured in (a), the expression level of pre-mRNA before and after administration of the compound represented by formula (I), the pharmaceutically acceptable salt thereof, or the 5 solvate of them, to determine that the compound represented by formula (I), the pharmaceutically acceptable salt thereof, or the solvate of them exerts an action to the mammal when the expression level of pre-mRNA after the administration increases.

[0009] (4) The method according to (3), wherein the pre-mRNA of which expression level is measured is pre-mRNA 10 of at least one gene selected from the genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5, or a homologous gene thereof. [0010] (5) The method according to (4), wherein the gene(s) are selected from DNAJB1, BZW1, NUP54, RIOK3, CDKN1B, STK17B, EIF4A1, and ID1. [0011] (6) The method according to (3), wherein in step (a), the expression level of pre-mRNA in samples obtained 15 from a subject before and after administration of the compound represented by formula (I), the pharmaceutically acceptable salt thereof, or the solvate of them, is measured. [0012] (7) The method according to (6), wherein the samples obtained from the subject are selected from hemocytes in peripheral blood, plasma, and serum. [0013] (8) A probe or primer for assaying an action of a compound represented by formula (I), a pharmaceutically 20 acceptable salt thereof, or a solvate of them to a mammal, which consists of a polynucleotide capable of hybridizing with a polynucleotide consisting of a nucleotide sequence of at least one gene selected from the genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5, or a homologous gene thereof, or a complementary sequence thereof. [0014] (9) The probe or primer according to (8), which is capable of detecting a genomic intron region or a part thereof in a gene listed in Table 1, Table 2, Table 3, Table 4 and Table 5, or which is capable of detecting a polynucleotide 25 lacking a part of a genomic exon region in a gene listed in Table 1, Table 2, Table 3, Table 4 and Table 5. [0015] (10) A reagent or kit for assaying an action of a compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a solvate of them to a mammal, which comprises the probe or the primer according to (8). [0016] (11) The method according to (1), wherein the detection of splicing defect comprises the steps of:

30 (f) measuring the expression level of an abnormal protein before and after administration of the compound represented by formula (I), the pharmaceutically acceptable salt thereof, or the solvate of them to a mammal; (g) comparing, based on the expression level measured in (f), the expression level of the abnormal protein before and after administration of the compound represented by formula (I), the pharmaceutically acceptable salt thereof or the solvate of them, to determine that the compound represented by formula (I), the pharmaceutically acceptable 35 salt thereof, or the solvate of them exerts an action to the mammal when the expression level of the abnormal protein after administration increases.

[0017] (12) The method according to (11), wherein the abnormal protein of which expression level is measured is a protein consisting of amino acids encoded by a polynucleotide of at least one gene selected from the genes listed in 40 Table 1 and Table 3, or a homologous gene thereof where splicing defect has been caused in the polynucleotide, or a protein consisting of amino acids encoded by a polynucleotide of at least one gene selected from the genes listed in Table 2, Table 4 and Table 5 or a homologous gene thereof where splicing defect has been caused in the polynucleotide. [0018] (13) The method according to (11), wherein the abnormal protein of which expression level is measured is a protein consisting of amino acids encoded by a polynucleotide of at least one gene selected from DNAJB1, BZW1, 45 NUP54, RIOK3, CDKN1B, STK17B, EIF4A1 and ID1 where splicing defect has been caused in the polynucleotide. [0019] (14) The method according to (11), wherein in step (f), the expression level of the abnormal protein in the samples obtained from a subject before and after administration of the compound represented by formula (I) or the pharmaceutically acceptable salt thereof or the solvate of them, is measured. [0020] (15) The method according to (14), wherein the samples obtained from the subject are selected from hemocytes 50 in peripheral blood, plasma, and serum. [0021] (16) An antibody against an abnormal protein consisting of amino acids encoded by a polynucleotide of at least one gene selected from the genes listed in Table 1, Table 2, Table 3, Table 4 and Table 5 where splicing defect has been caused in the polynucleotide, or a fragment thereof. [0022] (17) A reagent or kit for assaying an action of a compound represented by formula (I), a pharmaceutically 55 acceptable salt thereof, or a solvate of them to a mammal, comprising the antibody or the fragment thereof according to (16).

(18) Use of a probe or primer consisting of a polynucleotide capable of hybridizing with a polynucleotide consisting

5 EP 2 136 209 A1

of a nucleotide sequence of at least one gene selected from the genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5, and homologous genes thereof, or complementary sequences thereof, for assaying an action of a compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a solvate of them to a mammal. (19) Use of an antibody against a protein consisting of amino acids encoded by a polynucleotide of at least one 5 gene selected from the genes listed in Table 1, Table 2, Table 3, Table 4 and Table 5, or a fragment of the antibody, for assaying an action of a compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a solvate of them to a mammal.

[0023] According to the present invention, an action of the compound represented by formula (I) to a living body can 10 be confirmed using splicing defect in a cancerous or normal tissue of a cancer patient or normal tissue of a healthy individual, more specifically, the expression level of pre-mRNA or an abnormal protein as an index. For instance, when splicing defect is found in the cancerous or normal tissue of the cancer patient, more specifically, the expression level of pre-mRNA or the abnormal protein increases, it can be determined that the compound represented by formula (I) exerts the action in the body and that thus administration of the drug is no longer required or less amount of the drug 15 should be administrated. Further, when splicing defect is not found in the cancerous or normal tissue of the cancer patient, more specifically, the expression level of pre-mRNA or the abnormal protein exhibits the same amount as before the administration, it can be determined that the compound represented by formula (I) does not exert the action and further administration of the drug is required. Hence, according to the invention, by monitoring periodically the expression of pre-mRNA or the abnormal protein, the antitumor agent can be administered more effectively to the patient and a 20 minimally required amount of the drug can be administered to the patient. In particular, since the action of the compound represented by formula (I) can be judged by monitoring the expression level of pre-mRNA or the abnormal protein in samples obtained from normal tissue such as blood of the patient, it is an advantage that the action of the compound represented by formula (I) to the living body can be readily and reliably assessed.

25 BRIEF DESCRIPTION OF THE DRAWINGS

[0024]

Figure 1 shows accumulation of pre-mRNA of CDKN1B (p27) and CDKN1A (p21) in HeLa cells. 30 Figure 2 shows accumulation of pre-mRNA of DNAJB1, BZW1, SPAG5, RIOK3, NUP54, and BRD2 in HeLa cells. Figure 3 shows the expression of mRNA in whole blood (PBC) samples obtained from human peripheral blood. A: Results of samples obtained with the Tempus Blood RNA Tube. B: Results of samples obtained with the PAXgene Blood RNA Tube. Figure 4 shows expression of a protein translated from the pre-mRNA. 35 Figure 5 shows results measured expression of precursor genes (DNAJB1 and EIF4A1) in blood of nude mice to which human colon cancer cells were subcutaneously transplanted and the pladienolide derivative was administered. Figure 6 shows results measured expression of precursor genes (DNAJB1 and EIF4A1) in the tumor of nude mice to which human colon cancer cells were subcutaneously transplanted and the pladienolide derivative was administered. 40 Figure 7 shows a scatter diagram of the expression level of probe sets and genes of control cells, and standard deviation thereof. "A" represents the expression level and standard deviation of exons. "B" represents the expression level and standard deviation of genes.

DETAILED DESCRIPTION OF THE INVENTION 45 [0025] All technical terms, scientific terms and terminologies used in the present specification have the same meanings as those that are generally understood by those ordinary skilled in the art in the technical fields to which the present invention belongs, and are used merely for the purpose of explaining a specific embodiment but are not intended to make limitation. The present invention can be carried out in various embodiments as long as not departing from the 50 spirit thereof. All the prior art documents, published publications, patent publications and other patent documents cited in the present specification are incorporated into the present specification as references, and can be used for carrying out the present invention. [0026] The "halogen atom" used in the specification of the present application means a fluorine atom, a chlorine atom, a bromine atom and an iodine atom. Among them, for example, a fluorine atom, a chlorine atom or a bromine atom is 55 preferred, of which a fluorine atom or a chlorine atom is preferred. [0027] The "C1-22 alkyl group" used in the specification of the present application indicates a linear or branched alkyl group having 1 to 22 carbon atoms, such as methyl group, ethyl group, n-propyl group, iso-propyl group, n-butyl group, iso-butyl group, sec-butyl group, tert-butyl group, n-pentyl group, 1,1-dimethylpropyl group, 1,2-dimethylpropyl group,

6 EP 2 136 209 A1

2,2-dimethylpropyl group, 1-ethylpropyl group, n-hexyl group, 1-ethyl-2-methylpropyl group, 1,1,2-trimethylpropyl group, 1-propylpropyl group, 1-methylbutyl group, 2-methylbutyl group, 1,1-dimethylbutyl group, 1,2-dimethylbutyl group, 2,2- dimethylbutyl group, 1,3-dimethylbutyl group, 2,3-dimethylbutyl group, 2-ethylbutyl group, 2-methylpentyl group, 3-methylpentyl group, n-heptyl group, n-octyl group, n-nonyl group or n-decyl group; preferably a linear or branched alkyl group 5 having 1 to 6 carbon atoms, such as methyl group, ethyl group, n-propyl group, iso-propyl group, n-butyl group, iso-butyl group, sec-butyl group, tert-butyl group or n-pentyl group; and more preferably, for example, methyl group, ethyl group, propyl group, iso-propyl group, n-butyl group, iso-butyl group or tert-butyl group. [0028] The "unsaturated C2-22 alkyl group" used in the specification of the present application indicates a linear or branched alkenyl group having 2 to 22 carbon atoms or a linear or branched alkynyl group having 2 to 22 carbon atoms, 10 such as vinyl group, allyl group, 1-propenyl group, isopropenyl group, 2-methyl-1-propenyl group, 2-methyl-2-propenyl group, 1-butenyl group, 2-butenyl group, 3-butenyl group, 1-pentenyl group, 1-hexenyl group, 1,3-hexadienyl group, 1,5-hexadienyl group, ethynyl group, 1-propynyl group, 2-propynyl group, 1-butynyl group, 2-butynyl group, 3-butynyl group, 1-ethynyl-2-propynyl group, 2-methyl-3-butynyl group, 1-pentynyl group, 1-hexynyl group, 1,3-hexanediynyl group or 1,5-hexanediynyl group. It preferably indicates a linear or branched alkenyl group having 2 to 10 carbon atoms 15 or a linear or branched alkynyl group having 2 to 10 carbon atoms, such as vinyl group, allyl group, 1-propenyl group, 2-propenyl group, isopropenyl group, 3-methyl-2-butenyl group, 3,7-dimethyl-2,6-octadienyl group, ethynyl group, 1- propynyl group, 2-propynyl group, 1-butynyl group, 2-butynyl group, 3-butynyl group or 3-methyl-1-propynyl group. [0029] The "C6-14 aryl group" used in the specification of the present application means an aromatic cyclic hydrocarbon group having 6 to 14 carbon atoms, and a monocyclic group and condensed rings such as a bicyclic group and a tricyclic 20 group are included. Examples thereof include phenyl group, indenyl group, 1-naphthyl group, 2-naphthyl group, azulenyl group, heptalenyl group, indacenyl group, acenaphthyl group, fluorenyl group, phenalenyl group, phenanthrenyl group and anthracenyl group; and preferred examples include phenyl group, 1-naphthyl group and 2-naphthyl group. [0030] The "5- to 14-membered heteroaryl group" used in the specification of the present application means a monocyclic, bicyclic or tricyclic 5- to 14-membered aromatic heterocyclic group which contains one or more of hetero atoms 25 selected from the group consisting of nitrogen atom, sulfur atom and oxygen atom. Preferred examples thereof include nitrogen-containing aromatic heterocyclic groups such as pyrrolyl group, pyridyl group, pyridazinyl group, pyrimidinyl group, pyrazinyl group, triazolyl group, tetrazolyl group, benzotriazolyl group, pyrazolyl group, imidazolyl group, benz- imidazolyl group, indolyl group, isoindolyl group, indolizinyl group, purinyl group, indazolyl group, quinolyl group, isoqui- nolyl group, quinolizinyl group, phthalazinyl group, naphthyridinyl group, quinoxalinyl group, quinazolinyl group, cinnolinyl 30 group, pteridinyl group, imidazotriazinyl group, pyrazinopyridazinyl group, acridinyl group, phenanthridinyl group, car- bazolyl group, carbazolinyl group, perimidinyl group, phenanthrolinyl group, phenazinyl group, imidazopyridinyl group, imidazopyrimidinyl group, pyrazolopyridinyl group and pyrazolopyridinyl group; sulfur-containing aromatic heterocyclic groups such as thienyl group and benzothienyl group; and oxygen-containing aromatic heterocyclic groups such as furyl group, pyranyl group, cyclopentapyranyl group, benzofuryl group and isobenzofuryl group; aromatic heterocyclic groups 35 containing two or more different hetero atoms, such as thiazolyl group, isothiazolyl group, benzothiazolyl group, benz- thiadiazolyl group, phenothiazinyl group, isoxazolyl group, furazanyl group, phenoxazinyl group, oxazolyl group, isoxazoyl group, benzoxazolyl group, oxadiazolyl group, pyrazolooxazolyl group, imidazothiazolyl group, thienofuranyl group, furopyrrolyl group and pyridoxazinyl group; and preferred examples include thienyl group, furyl group, pyridyl group, pyridazyl group, pyrimidyl group and pyrazyl group. 40 [0031] The "3- to 14-membered non-aromatic heterocyclic group" used in the specification of the present application indicates a monocyclic, bicyclic or tricyclic 3- to 14-membered non-aromatic heterocyclic group which may contain one or more hetero atoms selected from the group consisting of nitrogen atom, sulfur atom and oxygen atom. Preferred examples thereof include aziridinyl group, azetidinyl group, pyrrolidinyl group, pyrrolyl group, piperidinyl group, piperazinyl group, homopiperidinyl group, homopiperazinyl group, imidazolyl group, pyrazolidyl group, imidazolidyl group, morpholyl 45 group, thiomorpholyl group, imidazolinyl group, oxazolinyl group, 2,5-diazabicyclo[2.2.1]heptyl group, 2,5-diazabicyclo [2.2.2]octyl group, 3,8-diazabicyclo[3.2.1]octyl group, 1,4-diazabicyclo[4.3.0]nonyl group, quinuclidyl group, tetrahydro- furan-yl group and tetrahydrothiophen-yl group. The non-aromatic heterocyclic groups also include groups derived from pyridone ring, and non-aromatic fused rings (e.g., a group derived from, for example, phthalimide ring or succinimide ring). [0032] The "C7-22 aralkyl group" used in the specification of the present application means a group corresponding to 50 the above-defined "C1-22 alkyl group" of which substitutable moiety is replaced by the above-defined "C6-14 aryl group". Specific examples thereof include benzyl group, phenethyl group, 3-phenylpropyl group, 4-phenylbutyl group, 1-naphthylmethyl group and 2-naphthylmethyl group; and preferred examples include aralkyl groups having 7 to 10 carbon atoms such as benzyl group and phenethyl group. [0033] The "5- to 14-membered heteroaralkyl group" used in the specification of the present application means a 55 group corresponding to the above-defined "C1-22 alkyl group" of which substitutable moiety is replaced by the above- defined "5- to 14-membered heteroaryl group". Specific examples thereof include thienylmethyl group, furylmethyl group, pyridylmethyl group, pyridazylmethyl group, pyrimidylmethyl group and pyrazylmethyl group; and preferred examples include thienylmethyl group, furylmethyl group and pyridylmethyl group.

7 EP 2 136 209 A1

[0034] The "C3-14 cycloalkyl group" used in the specification of the present application indicates a cycloalkyl group having 3 to 14 carbon atoms, and suitable examples thereof include cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group and cyclooctyl group; and preferred examples include cyclopentyl group, cyclohexyl group, cycloheptyl group and cyclooctyl group. 5 [0035] The "C4-9 cycloalkyl alkyl group" used in the specification of the present application means a group corresponding to the above-defined "C1-22 alkyl group" of which substitutable moiety is replaced by the above-defined "C3-14 cycloalkyl group". Specific examples thereof include cyclopropylmethyl group, cyclobutylmethyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group and cyclooctylmethyl group; and preferred example include cyclopropylmethyl group, cyclobutylmethyl group and cyclopentylmethyl group. 10 [0036] The "C1-22 alkoxy group" used in the specification of the present application means a group corresponding to the above-defined "C1-22 alkyl group" to which end an oxygen atom is bonded. Suitable examples thereof include methoxy group, ethoxy group, n-propoxy group, iso-propoxy group, n-butoxy group, iso-butoxy group, sec-butoxy group, tert- butoxy group, n-pentyloxy group, iso-pentyloxy group, sec-pentyloxy group, n-hexoxy group, iso-hexoxy group, 1,1- dimethylpropyloxy group, 1,2-dimethylpropyloxy group, 2,2-dimethylpropoxy group, 1-methyl-2-ethylpropoxy group, 1- 15 ethyl-2-methylpropoxy group, 1,1,2-trimethylpropoxy group, 1,2,2-trimethylpropoxy group, 1,1-dimethylbutoxy group, 1,2-dimethylbutoxy group, 2,2-dimethylbutoxy group, 2,3-dimethylbutyloxy group, 1,3-dimethylbutoxy group, 2-ethylbu- toxy group, 2-methylpentoxy group, 3-methylpentyloxy group and hexyloxy group; and preferred examples include methoxy group, ethoxy group, n-propoxy group, iso-propoxy group, iso-butoxy group and 2,2-dimethylpropyloxy group. [0037] The "unsaturated C2-22 alkoxy group" used in the specification of the present application means a group cor- 20 responding to the above-defined "unsaturated C2-22 alkyl group" to which end an oxygen atom is bonded. Suitable examples thereof include vinyloxy group, allyloxy group, 1-propenyloxy group, 2-propenyloxy group, isopropenyloxy group, 2-methyl-1-propenyloxy group, 2-methyl-2-propenyloxy group, 1-butenyloxy group, 2-butenyloxy group, 3-butenyloxy group, 1-pentenyloxy group, 1-hexenyloxy group, 1,3-hexadienyloxy group, 1,5-hexadienyloxy group, propargyloxy group and 2-butynyloxy group; and preferred examples include allyloxy group, propargyloxy group and 2-butynyloxy 25 group. [0038] The "C6-14 aryloxy group" used in the specification of the present application means a group corresponding to the above-defined "C6-14 aryl group" to which end an oxygen atom is bonded. Specific examples thereof include phenyloxy group, indenyloxy group, 1-naphthyloxy group, 2-naphthyloxy group, azulenyloxy group, heptalenyloxy group, indace- nyloxy group, acenaphthyloxy group, fluorenyloxy group, phenalenyloxy group, phenanthrenyloxy group and anthrace- 30 nyloxy group; and preferred examples include phenyloxy group, 1-naphthyloxy group and 2-naphthyloxy group. [0039] The "C7-22 aralkyloxy group" used in the specification of the present application means a group corresponding to the above-defined "C7-22 aralkyl group" to which end an oxygen atom is bonded. Specific examples thereof include benzyloxy group, phenethyloxy group, 3-phenylpropyloxy group, 4-phenylbutyloxy group, 1-naphthylmethyloxy group and 2-naphthylmethyloxy group; and preferred examples include benzyloxy group. 35 [0040] The "5- to 14-membered heteroaralkyloxy group" used in the specification of the present application means a group corresponding to the above-defined "5- to 14-membered heteroaralkyl group" to which end an oxygen atom is bonded. Specific examples thereof include thienylmethyloxy group, furylmethyloxy group, pyridylmethyloxy group, pyridazylmethyloxy group, pyrimidylmethyloxy group and pyrazylmethyloxy group; and preferred examples include thienylmethyloxy group, furylmethyloxy group and pyridinylmethyloxy group. 40 [0041] The "5- to 14-membered heteroaryloxy group" used in the specification of the present application means a group corresponding to the above-defined "5- to 14-membered heteroaryl group" to which end an oxygen atom is bonded. Specific examples thereof include pyrrolyloxy group, pyridyloxy group, pyridazinyloxy group, pyrimidinyloxy group, pyrazi- nyloxy group, triazolyloxy group, tetrazolyloxy group, benzotriazolyloxy group, pyrazolyloxy group, imidazolyloxy group, benzimidazolyloxy group, indolyloxy group, isoindolyloxy group, indolizinyloxy group, purinyloxy group, indazolyloxy 45 group, quinolyloxy group, isoquinolyloxy group, quinolizyloxy group, phthalazyloxy group, naphthyridinyloxy group, quinoxalyloxy group, quinazolinyloxy group, cinnolinyloxy group, pteridinyloxy group, imidazotriazinyloxy group, pyrazinopyridazinyloxy group, acridinyloxy group, phenanthridinyloxy group, carbazolyloxy group, carbazolinyloxy group, perimidinyloxy group, phenanthrolinyloxy group, phenazinyloxy group, imidazopyridinyloxy group, imidazopyrimidinyloxy group, pyrazolopyridinyloxy group, pyrazolopyridinyloxy group, thienyloxy group, benzothienyloxy group, furyloxy group, 50 pyranyloxy group, cyclopentapyranyloxy group, benzofuryloxy group, isobenzofuryloxy group, thiazolyloxy group, iso- thiazolyloxy group, benzothiazolyloxy group, benzothiadiazolyloxy group, phenothiazinyloxy group, isoxazoyloxy group, furazanyloxy group, phenoxazinyloxy group, oxazolyloxy group, isoxazolyloxy group, benzoxazolyloxy group, oxadia- zolyloxy group, pyrazolooxazolyloxy group, imidazothiazolyloxy group, thienofuranyloxy group, furopyrrolyloxy group and pyridoxazinyloxy group; and preferred examples include thienyloxy group, pyridyloxy group, pyrimidyloxy group and 55 pyrazyloxy group. [0042] The "aliphatic C2-22 acyl group" used in the specification of the present application means a group corresponding to the above-defined "C1-22 alkyl group" or "unsaturated C2-22 alkyl group" to which end a carbonyl group is bonded. Examples thereof include acetyl group, propionyl group, butyryl group, iso-butyryl group, valeryl group, iso-valeryl group,

8 EP 2 136 209 A1

pivaloyl group, caproyl group, decanoyl group, lauroyl group, myristoyl group, palmitoyl group, stearoyl group, arachidoyl group, acryloyl group, propiol group, crotonyl group, iso-crotonyl group, olenoyl group and linolenoyl group; and preferred examples include aliphatic acyl groups having 2 to 6 carbon atoms, such as acetyl group, propionyl group, butyryl group, iso-butyryl group and acryloyl group. 5 [0043] The "aromatic C7-15 acyl group" used in the specification of the present application means a group corresponding to the above-defined "C6-14 aryl group" or "5- to 14-membered heteroaryl group" to which end a carbonyl group is bonded. Examples thereof include benzoyl group, 1-naphthoyl group, 2-naphthoyl group, picolinoyl group, nicotinoyl group, isonicotinoyl group, furoyl group and thiophenecarbonyl group; and preferred examples include benzoyl group, picolinoyl group, nicotinoyl group and isonicotinoyl group. 10 [0044] The "C1-22 alkylsulfonyl group" used in the specification of the present application means a group corresponding to the above-defined "C1-22 alkyl group" to which a sulfonyl group is bound. Specific examples thereof include methylsulfonyl group, ethylsulfonyl group, n-propylsulfonyl group and iso-propylsulfonyl group; and preferred examples include methylsulfonyl group.

[0045] The "C6-14 arylsulfonyl group" used in the specification of the present application means a group corresponding 15 to the above-defined "C6-14 aryl group" to which a sulfonyl group is bound. Specific examples thereof include benzenesulfonyl group, 1-naphthalenesulfonyl group and 2-naphthalenesulfonyl group; and preferred examples include benzenesulfonyl group. [0046] The "aliphatic C2-22 acyloxy group" used in the specification of the present application means a group corresponding to the above-defined "aliphatic C2-22 acyl group" to which end an oxygen atom is bonded. Specific examples 20 thereof include acetoxy group, propionyloxy group and acryloxy group; and preferred examples include acetoxy group and propionyloxy group. [0047] The "C2-22 alkoxycarbonyl group" used in the specification of the present application means a group corresponding to the above-defined "C1-22 alkoxy group" to which end a carbonyl group is bonded. Examples thereof include methoxycarbonyl group, ethoxycarbonyl group, n-propoxycarbonyl group, iso-propoxycarbonyl group, n-butoxycarbonyl 25 group, iso-butoxycarbonyl group, sec-butoxycarbonyl group and tert-butoxycarbonyl group; and preferred examples include ethoxycarbonyl group, iso-propoxycarbonyl group and tert-butoxycarbonyl group. [0048] The "unsaturated C3-22 alkoxycarbonyl group" used in the specification of the present application means a group corresponding to the above-defined "unsaturated C2-22 alkoxy group" to which end a carbonyl group is bonded. Examples thereof include vinyloxycarbonyl group, allyloxycarbonyl group, 1-propenyloxycarbonyl group, isopropeny- 30 loxycarbonyl group, propargyloxycarbonyl group and 2-butynyloxycarbonyl group; and preferred examples include allyloxycarbonyl group. [0049] The "C1-22 alkylthio group" used in the specification of the present application means a group corresponding to the above-defined "C1-22 alkyl group" to which end a sulfur atom is bonded. Examples thereof include methylthio group, ethylthio group, n-propylthio group and iso-propylthio group; and preferred examples include methylthio group 35 or ethylthio group. [0050] The "C1-22 alkylsulfinyl group" used in the specification of the present application means a group corresponding to the above-defined "C1-22 alkyl group" to which end a sulfinyl group is bonded. Examples thereof include methylsulfinyl group, ethylsulfinyl group, n-propylsulfinyl group and iso-propylsulfinyl group; and preferred examples include meth- anesulfinyl group or ethanesulfinyl group. 40 [0051] The "C1-22 alkylsulfonyloxy group" used in the specification of the present application means a group corresponding to the above-defined "C1-22 alkylsulfonyl group" to which end an oxygen atom is bonded. Examples thereof include methylsulfonyloxy group, ethylsulfonyloxy group, n-propylsulfonyloxy group and iso-propylsulfonyloxy group; and preferred examples include methylsulfonyloxy group. [0052] The substituent of the phrase "an optionally substituted" used in the specification of the present application 45 may be one or more groups selected from:

(1) a halogen atom, (2) a hydroxyl group, (3) a thiol group, 50 (4) a nitro group, (5) a nitroso group, (6) a cyano group, (7) a carboxyl group, (8) a hydroxysulfonyl group, 55 (9) a amino group, (10) a C1-22 alkyl group (for example, methyl group, ethyl group, n-propyl group, iso-propyl group, n-butyl group, iso-butyl group, sec-butyl group and tert-butyl group), (11) an unsaturated C2-22 alkyl group (for example, vinyl group, allyl group, 1-propenyl group, 2-propenyl group,

9 EP 2 136 209 A1

isopropenyl group, ethynyl group, 1-propynyl group, 2-propynyl group, 1-butynyl group, 2-butynyl group and 3- butynyl group), (12) a C6-14 aryl group (for example, phenyl group, 1-naphthyl group and 2-naphthyl group), (13) a 5- to 14-membered heteroaryl group (for example, thienyl group, furyl group, pyridyl group, pyridazyl group, 5 pyrimidyl group and pyrazyl group), (14) a 3- to 14-membered non-aromatic heterocyclic group (for example, aziridinyl group, azetidyl group, pyrrolidinyl group, pyrrolyl group, piperidinyl group, piperazinyl group, homopiperidinyl group, homopiperazinyl group, imidazolyl group, pyrazolidyl group, imidazolidyl group, morpholyl group, thiomorpholyl group, imidazolinyl group, oxazolinyl group and quinuclidyl group), 10 (15) a C3-14 cycloalkyl group (for example, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group and cyclooctyl group), (16) a C1-22 alkoxy group (for example, methoxy group, ethoxy group, n-propoxy group, iso-propoxy group, sec- propoxy group, n-butoxy group, iso-butoxy group and tert-butoxy group), (17) an unsaturated C2-22 alkoxy group (for example, vinyloxy group, allyloxy group, 1-propenyloxy group, 2-prope- 15 nyloxy group, isopropenyloxy group, ethynyloxy group, 1-propynyloxy group, 2-propynyloxy group, 1-butynyloxy group and 2-butynyloxy group), (18) a C6-14 aryloxy group (for example, phenyloxy group, 1-naphthyloxy group and 2-naphthyloxy group), (19) a C7-22 aralkyloxy group (for example, benzyloxy group, phenethyloxy group, 3-phenylpropyloxy group, 4- phenylbutyloxy group, 1-naphthylmethyloxy group and 2-naphthylmethyloxy group), 20 (20) a 5- to 14-membered heteroaralkyloxy group (for example, thienylmethyloxy group, furylmethyloxy group, pyridylmethyloxy group, pyridazylmethyloxy group, pyrimidylmethyloxy group and pyrazylmethyloxy group), (21) a 5- to 14-membered heteroaryloxy group (for example, thienyloxy group, furyloxy group, pyridyloxy group, pyridazyloxy group, pyrimidyloxy group and pyrazyloxy group), (22) an aliphatic C2-22 acyl group (for example, acetyl group, propionyl group, butyryl group, iso-butyryl group, valeryl 25 group, iso-valeryl group, pivalyl group, caproyl group, decanoyl group, lauroyl group, myristoyl group, palmitoyl group, stearoyl group, arachidoyl group, acryl group, propiol group, crotonyl group, iso-crotonyl group, olenoyl group and linolenoyl group), (23) an aromatic C7-15 acyl group (for example, benzoyl group, 1-naphthoyl group and 2-naphthoyl group), (24) an aliphatic C2-22 acyloxy group (for example, acetoxy group, propionyloxy group and acryloxy group), 30 (25) a C2-22 alkoxycarbonyl group (for example, methoxycarbonyl group, ethoxycarbonyl group, n-propoxycarbonyl group, iso-propoxycarbonyl group, n-butoxycarbonyl group, iso-butoxycarbonyl group, sec-butoxycarbonyl group and tert-butoxycarbonyl group), (26) an unsaturated C3-22 alkoxycarbonyl group (for example, vinyloxycarbonyl group, allyloxycarbonyl group, 1- propenyloxycarbonyl group, 2-propenyloxycarbonyl group, isopropenyloxycarbonyl group, propargyloxycarbonyl 35 group and 2-butynyloxycarbonyl group), (27) a C1-22 alkylthio group (for example, methylthio group, ethylthio group, n-propylthio group and iso-propylthio group), (28) a C1-22 alkylsulfinyl group (for example, methylsulfinyl group, ethylsulfinyl group, n-propylsulfinyl group and iso- propylsulfinyl group), 40 (29) a C1-22 alkylsulfonyl group (for example, methylsulfonyl group, ethaylsulfonyl group, n-propanesulfonyl group and iso-propanesulfonyl group), (30) a C6-14 arylsulfonyl group (for example, benzenesulfonyl group, 1-naphthalenesulfonyl group and 2-naphthalenesulfonyl group), (31) a C1-22 alkylsulfonyloxy group (for example, methylsulfonyloxy group, ethylsulfonyloxy group, n-propylsulfony- 45 loxy group and iso-propanesulfonyloxy group), (32) carbamoyl group, and (33) formyl group.

Among them, a preferred example is an amino group, a C1-22 alkyl group, an unsaturated C2-22 alkyl group, a C6-14 aryl 50 group, a 5- to 14-membered heteroaryl group, a 3- to 14-membered non-aromatic heterocyclic group and a C3-14 cycloalkyl group, and a more preferred example is an amino group, a C1-22 alkyl group, a 3- to 14-membered nonaromatic heterocyclic group and a C3-14 cycloalkyl group. The above-mentioned (9) amino group and (31) carbamoyl group as the substituent in "an optionally substituted" may each be further substituted with one or two of a C1-22 alkyl group, an unsaturated C2-22 alkyl group or a C6-14 aryl group. 55 [0053] In the present specification, the chemical formula of the compound according to the present invention is illus- trated as a planimetric chemical formula for convenience but the compound can include certain isomers drawn from the chemical formula. The present invention can include all isomers and mixtures of the isomers such as a geometric isomer which is generated from the configuration of the compound, an optical isomer based on an asymmetric carbon, a rotamer,

10 EP 2 136 209 A1

a stereoisomer and a tautomer. The present invention is not limited to the expediential description of the chemical formula, and can include either of isomers or a mixture thereof. Accordingly, when the compound according to the present invention has an asymmetric carbon in the molecule, and its optically active substance and racemate exist, any one is included. Further, when polymorphic crystals exist, the crystal form according to the present invention is not specifically 5 limited to one form, and any one of the crystal forms may be single or a mixture of the crystal forms. [0054] The "pharmaceutically acceptable salt" used in the present invention is not particularly restricted as long as it can form a salt with the compound represented by formula (I), and is pharmaceutically acceptable. Preferred examples thereof include halide hydroacid salt such as hydrochloric acid salt, hydrobromic acid salt, hydroiodic acid salt; inorganic acid salt such as sulphic acid salt, nitric acid salt, perchloric acid salt, phosphoric acid salt, carbonic acid salt, bicarbonic 10 acid salt; organic carboxylic acid salt such as acetic acid salt, trifluoroacetic acid salt, maleic acid salt, tartaric acid salt, fumaric acid salt, citric acid salt; organic sulfonic acid salt such as methanesulfonic acid salt, trifluoro methanesulfonic acid salt, ethanesulfonic acid salt, benzenesulfonic acid salt, toluenesulfonic acid salt, camphorsulfonic acid salt; amino acid salt such as aspartic acid salt, glutamic acid salt; quaternary amine salt; alkaline metal salt such as sodium salt, potassium salt; and alkaline earth metal salt such as magnesium salt, calcium salt. 15 [0055] The "solvate" used in the present invention is not particularly restricted as long as it can form a solvate with the compound represented by formula (I) or the salt thereof, and is pharmaceutically acceptable. Preferred examples include hydrate, alcoholate such as ethanolate, and etherate. [0056] The present invention also includes a metabolite generated by degradation of the compound represented by formula (I) within a living body, as well as a prodrug of the compound represented by formula (I) and the salt thereof. 20 The "prodrug" used herein means an inert substance to which "an active moiety of a drug" (meaning "drug" corresponding to a prodrug) has been chemically modified, for the purpose of improvement of bioavailability and reduction of a side effect. After absorbed, it is metabolized into the active moiety in vivo and exerts an action. Accordingly, the term "prodrug" refers to any compound having a lower intrinsic activity than the corresponding "drug", which is, once administrated to a biological system, converted into the "drug" substance via a spontaneous chemical reaction, enzyme catalyzed reaction 25 or metabolic reaction. Examples of such prodrugs include various prodrugs, for example, compounds produced by acylation, alkylation, phosphorylation, boration, carbonation, esterification, amidation, or urethanation of a functional group such as an amino, hydroxyl, or carboxyl group in the compound represented by formula (I). However, it should be noted that the exemplified prodrugs are not comprehensive but are merely typical, and other conventional various prodrugs can be prepared by a conventional method by a person having ordinary skill in the art from the compound 30 represented by formula (I). [0057] When the compound represented by formula (I) is administrated to a mammal in the method according to the present invention, the compound represented by formula (I) may be formulated by known methods. Conventional carriers are used for formulation, and the pharmaceutical products are prepared by conventional methods. Namely, when a solid formulation for oral use is prepared, a filler is added to the main drug, and if necessary, a binder, a disintegrant, a 35 lubricant, a colorant, a flavoring agent and the like are added thereto, and then tablets, coated tablets, granules, powders, capsules and the like are prepared by conventional methods. It is needless to say that sugar coating, gelatin coating or suitable coating may be conducted on the tablet and granule, if necessary. When the compounds are formulated as an injection, a pH regulator, a buffer, a stabilizer, a solubilizer and the like are added to the main drug, if necessary, to prepare an subcutaneous, intramuscular, intra-articular or intravenous injection according to conventional procedures. 40 When the compound represented by formula (I) is administered as a therapeutic or preventive agent for various diseases, it may be orally administered as tablets, powders, granules, capsules, syrups and the like, and may be parenterally administered as a spray, a suppository, an injection, a topical preparation or an infusion. Although the dose remarkably varies according to the severity of symptom, age, the kind of disease etc., approximately 1 mg to 100 mg per day for an adult is administered in general at one time or several times per day. 45 [0058] When the expression level of pre-mRNA of the genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5 or homologous genes thereof, preferably the genes listed in Table 1 and Table2 or homologous genes thereof as well as an abnormal protein generated by splicing defect of the gene is monitored in the method according to the present invention, the expression level may be preferably monitored before administration of the compound represented by formula (I), followed by another monitoring at 3, 6, 8, 24, or 48 hours after the administration. In a preferred embodiment, 50 follow-up monitoring of the expression level is carried out at the earliest three hours after the administration of the compound represented by formula (I). [0059] Upon implementing the method according to the present invention the splicing defect can be detected using an increase in the expression level of pre-mRNA or the abnormal protein caused by the splicing defect as an index. [0060] According to a first aspect of the invention, a method for assaying the action of the compound represented by 55 formula (I), using the increase in the expression level of pre-mRNA as an index (invention (3)) is provided. [0061] In step (a), cancer tissue or normal tissue such as hemocytes in peripheral blood, platelets, and serum can be taken from the mammal subjected to the assay and pre-mRNA samples can be prepared from the obtained samples to quantify the expression level of pre-mRNA. Preparation of pre-mRNA is well known (for example, "Molecular Cloning,

11 EP 2 136 209 A1

A Laboratory Manual 3d ed. "(Cold Spring Harbor Press (2001)), and required devices, instruments, and reagents therefor are commercially available. Hence those skilled in the art may prepare pre-mRNA with no difficulties using the devices, apparatuses, and reagents as needed. [0062] Measurement of the expression level of pre-mRNA in step (a) can be performed with any method selected 5 from a Northern blot method, a dot blot method, an RT-PCR method, and a microarray (preferably, Human Exon 1.0 ST Array). The principles of these methods and how to carry out these methods are well-known, and the required devices and apparatuses therefor are commercially available. Moreover, in Examples below, an example in which the expression level of pre-mRNA is measured with these methods will be described. Those skilled in the art can measure the expression level of pre-mRNA with no difficulties using the Northern blot method, the dot blot method, the RT-PCR method, and 10 the microarray. In the measurement of the expression level of pre-mRNA in step (a), preferably, the microarray can be used. [0063] For the measurement of the expression level of pre-mRNA in step (a), a probe and a primer which consist of a polynucleotide capable of hybridizing with nucleotide sequences of genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5 and homologous genes thereof, preferably genes listed in Table 1 and Table2 or homologous genes thereof, 15 or their complementary sequences can be employed as a detection marker. [0064] Any probe and primer according to the present invention may be employed as long as it can detect the expression of pre-mRNA (including a part thereof) of the genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5 and homologous genes thereof, preferably the genes listed in Table 1 and Table2 or homologous genes thereof. The probe and the primer according to the present invention refers to a polymer consisting of bases or base pairs such as deox- 20 yribonucleic acid (DNA) or ribonucleic acid (RNA). It has been known that double stranded cDNA can be used in tissue in situ hybridization, and the probe and the primer according to the present invention include such double stranded cDNA. Particularly preferred RNA probe and primer for detecting RNA in tissue include RNA probes (riboprobe). [0065] The probe and the primer according to the present invention includes a probe or a primer which consists of a polynucleotide comprising a nucleotide sequence of at least 10, preferably at least 15, more preferably at least 20, further 25 preferably at least 25 continuous nucleotides of the genes listed in Table 1, Table 2, Table 3, Table 4 and Table 5, and homologous genes thereof, preferably genes listed in Table 1 and Table2 or homologous genes thereof, or complementary sequences thereof as well as all mutated polynucleotide sequences thereof. The probe and the primer according to the present invention include a probe or a primer which consists of a polynucleotide comprising a nucleotide sequence of 10 to 50 or 10 to 30 continuous nucleotides, 15 to 50 or 15 to 30 continuous nucleotides, 20 to 50 or 20 to 30 continuous 30 nucleotides, 25 to 50 or 25 to 30 continuous nucleotides, of the genes listed in Table 1, Table 2, Table 3, Table 4 and Table 5, and homologous genes thereof, preferably the genes listed in Table 1 and Table2 or homologous genes thereof or mutated polynucleotide sequences thereof. [0066] The probe and the primer according to the present invention may be at least 10 bases in length, preferably at least 15 bases in length, more preferably at least 20 bases in length, further preferably at least 25 bases in length. The 35 probe and the primer according to the present invention may also be 10 to 50 bases or 10 to 30 bases in length, 15 to 50 bases or 15 to 30 bases in length, 20 to 50 bases or 20 to 30 bases in length, 25 to 50 bases or 25 to 30 bases in length. [0067] According to the preferred embodiment of the probe and the primer according to the present invention, there are provided the probe and the primer having 15 to 30 bases in length for assaying the action of the compound represented by formula (I) to the mammals, which consist of a polynucleotide comprising at least 10, preferably at least 15, more 40 preferably at least 20, further preferably at least 25 continuous nucleotides of a polynucleotide sequence of the genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5 or homologous genes thereof, preferably the genes listed in Table1 and Table2 or homologous genes thereof, as well as all mutated sequences thereof, and which are capable of hybridizing with a polynucleotide sequence of the genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5 or homologous genes thereof, preferably the genes listed in Table 1 and Table2 or homologous genes thereof. 45 [0068] According to a preferred aspect of the probe and the primer according to the present invention, there are provided a probe and a primer which are capable of hybridizing with a more distinct region within a nucleotide sequence of the genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5 or homologous genes thereof, preferably the genes listed in Table 1 and Table2 or homologous genes thereof. The above probe and primer allow more precise detection of the action of the compound represented by formula (I) to the mammal. 50 [0069] The probe according to the present invention can be chemically synthesized based on the nucleotide sequence of the gene subjected to be detected. Preparation of the probes is well known and can be carried out in accordance with, for example, "Molecular Cloning, A Laboratory Manual 2nd ed." (Cold Spring Harbor Press (1989)), "Current Protocols in Molecular Biology" (John Wiley & Sons (1987-1997)). [0070] The primers according to the present invention can be used as a primer set comprising of two or more types 55 of the primers. [0071] The primer and the primer set according to the present invention can be used as a primer and a primer set in accordance with a conventional method in a known method for detecting the target gene using a nucleic acid amplification method such as a PCR method, a RT-PCR method, a real-time PCR method, and an in situ PCR method.

12 EP 2 136 209 A1

[0072] The primer set according to the present invention can be selected such that the nucleotide sequence of the target gene can be amplified with the nucleic acid amplification method such as the PCR method. The nucleic acid amplification method is well known and selection of the primer pair therein is obvious for those skilled in the art. For example, in the PCR method, the primers can be selected such that one of two primers (a primer pair) undergoes base 5 pairing with the plus strand of the double stranded DNA of the gene subjected to be detected whereas the other of the primers undergoes base pairing with the minus strand of the double stranded DNA, as well as an extending strand extended with one primer can be paired with the other primer. In a LAMP method (WO00/28082), three regions from the 3’ terminus termed F3c, F2c and F1c, and three regions from the 5’ terminus termed B1, B2 and B3 are respectively defined for the gene subjected to be detected. Four types of primers can be designed using these six regions. 10 [0073] The primer according to the present invention may be chemically synthesized based on the nucleotide sequence of the gene subjected to be detected. Preparation of the primer is well known and can be carried out in accordance with, for example, "Molecular Cloning, A Laboratory Manual 2nd ed." (Cold Spring Harbor Press (1989)), "Current Protocols in Molecular Biology" (John Wiley & Sons (1987-1997)). [0074] Table 1, Table 2, Table 3, Table 4, and Table 5 describe information specifying the genes and homologous 15 genes thereof listed in these tables. Accordingly those skilled in the art can obtain information on the nucleotide sequence of the subject gene to be detected based on the information described in Table 1, Table 2, Table 3, Table 4, and Table 5 to design the probe and primer based thereon. [0075] In addition, the genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5 are known genes and probes and primers for detecting them are commercially available individually or as a detection kit or detection array. 20 [0076] The term "to hybridize" used in the specification of the present application means to hybridize with a target polynucleotide under stringent conditions. A specific example of the polynucleotide which hybridizes under stringent conditions includes a polynucleotide having at least 70% or more, preferably 80% or more, more preferably 85% or more, further preferably 90% or more, further more preferably 95% or more, particularly preferably 98% or more, and most preferably 99% or more homology to the target polynucleotide when the homology is calculated by a homology 25 search software, such as FASTA, BLAST, Smith-Waterman (Meth. Enzym., 164, 765, (1988)), using default parameters. Further, hybridization "under stringent conditions" can be performed, for example, by a method of carrying out the reaction at a temperature of 40°C to 70°C, preferably at a temperature of 60°C to 65°C, in a hybridization buffer solution generally used by those skilled in the art, and carrying out washing in a washing solution at a salt concentration of 15 to 300 mmol/L, preferably at 15 to 60 mmol/L. The temperature and salt concentration can be appropriately adjusted depending 30 on the length of the probe to be used. Further the hybridized product can be washed under conditions in 0.2x or 2x SSC and 0.1% SDS at a temperature of 20°C to 68°C. Whether stringent (high stringency) or mild (low stringency) conditions is used depends on a difference in salt concentrations and temperatures while the washing process. In cases where the difference in hybridizing depends on the salt concentration, the washing process can be carried out in 0.2x SSC and 0.1% SDS as a stringent washing buffer (high stringency wash buffer) and 2x SSC and 0.1% SDS as a mild washing 35 buffer (low stringency wash buffer). Also, in cases where the difference in hybridizing depends on the temperature, the washing process may be carried out at 68°C for stringent conditions, at 42°C for medium (moderate stringency) conditions, or at room temperature (20-25°C) for mild conditions, but 0.2x SSC and 0.1% SDS are used in all the cases. [0077] When pre-hybridization is carried out, it is carried out under the same condition as in hybridization, but pre (preliminary)-washing is not necessarily carried out under the same condition as in hybridization. 40 [0078] The "homologous gene" used in the specification of the present application means a gene encoding a protein functionally equivalent to a protein encoded by a certain gene. Whether it is "functionally equivalent" or not can be determined by evaluating if the protein has functions equivalent to biological phenomena or functions related to the expression of the gene. Such a gene encoding the functionally equivalent protein includes not only the so-called homologous gene but also a gene with polymorphism and a gene having a mutation without affecting the function. 45 [0079] Examples of the homologous gene include genes which have a nucleotide sequence of a certain gene wherein one or more (preferably one to several, or 1, 2, 3 or 4) nucleotides are inserted, substituted or deleted, or added to one or both termini, and which encode the functionally equivalent protein. [0080] Examples of the homologous gene also include genes which encode an amino acid sequence encoded by a certain gene wherein one or more amino acids are inserted, substituted, or deleted, or added to one or both termini 50 (modified amino acid sequence), and which encode the functionally equivalent protein. [0081] "One or more amino acids are inserted, substituted, or deleted, or added to one or both termini" used in the specification of the present application means that a modification is made by a known technical method such as a site specific mutagenesis method or by substitution of several amino acids as in naturally occurring mutation. [0082] The "modified amino acid sequence" used in the specification of the present application can be an amino acid 55 sequence wherein, for example, 1 to 30 amino acids, preferably 1 to 20 amino acids, more preferably 1 to 9 amino acids, further preferably 1 to 5 amino acids, particularly preferably 1 to 2 amino acids have been inserted, substituted, or deleted, or added to one or both termini. Preferably, the modified amino acid sequence may be an amino acid sequence having one or more (preferably one or several or 1, 2, 3, or 4) conservative substitutions.

13 EP 2 136 209 A1

[0083] The term "conservative substitution" is used herein to mean that one or more amino acid residues are substituted with other chemically similar amino acid residues, so as not to substantially modify the functions of a protein. Examples of such conservative substitution include a case where a certain hydrophobic residue is substituted with another hydrophobic residue and a case where a certain polar residue is substituted with another polar residue having the same 5 electric charge. Such functionally similar amino acids that can be used in such substitution are known as every amino acid types in the present technical field. Specific examples of a nonpolar (hydrophobic) amino acid include alanine, valine, isoleucine, leucine, proline, tryptophan, phenylalanine, and methionine. Examples of a polar (neutral) amino acid include glycine, serine, threonine, tyrosine, glutamine, asparagine, and cysteine. Examples of a (basic) amino acid having a positive charge include arginine, histidine, and lysine. Examples of an (acidic) amino acid having a negative 10 charge include aspartic acid and glutamic acid. [0084] In cases where the first aspect of the present invention is carried out using a cancer tissue and its surrounding tissue as assay samples, the action of the compound represented by formula (I) can be assayed preferably by using the expression level of pre-mRNA of the genes listed in Table 1 and Table 3 or homologous genes thereof as an index. Measurement of the expression level of the pre-mRNA in cases where the cancer tissue and the surrounding tissue are 15 used as the samples, the microarray can be preferably used. [0085] In cases where the first aspect of the present invention is carried out using a normal tissue, in particular peripheral blood and whole blood as the assay samples, the action of the compound represented by formula (I) can be assayed preferably by using the expression level of pre-mRNA of the genes listed in Table 2, Table 4, and Table 5, or homologous genes thereof as an index. Measurement of the expression level of the pre-mRNA in cases where the 20 peripheral blood and whole blood are used as the samples, the microarray can be preferably used. [0086] According to a second aspect of the present invention, a method for assaying the action of the compound represented by formula (I), using an increase in the expression level of an abnormal protein expressed resulting from splicing defect of pre mRNA (invention (11)) is provided. [0087] The abnormal protein measured in step (f) is an abnormal protein resulting from splicing defect of the genes 25 listed Table 1, Table 2, Table 3, Table 4, and Table 5, or homologous genes thereof. Table 1, Table 2, Table 3, Table 4, and Table 5 describe information specifying the genes listed in these tables and homologous genes thereof. [0088] In step (f), samples are taken from a cancer tissue or normal tissue such as hemocytes in peripheral blood, plasma, and serum from a mammal subjected to the assay. Measurement of the expression level of the abnormal protein may be carried out with the collected samples as they are or a protein extracted therefrom. Extraction of the protein is 30 well known (for example, Campa, M.J. et al. Cancer Res. 63, 1652-1656, 2003), and devices, instruments, and reagents necessary for carrying out the extraction are commercially available. Hence those skilled in the art may extract the protein with no difficulties using such the commercially available devices, apparatuses, and reagents as needed. [0089] The measurement of the expression level of the abnormal protein in step (f) can be carried out with a method selected from a fluorescent antibody method, an enzyme immunoassay (ELISA) method, a radioimmunoassay (RIA) 35 method, a Western blot method and an immunostaining (immunohistochemistry) method. The principle and implemen- tation procedures of these methods are well known and devices and instruments necessary for carrying out the methods are commercially available. Furthermore, in Examples below, an example in which the expression level of pre-mRNA is measured with those methods will be described. Those skilled in the art may measure the expression level of pre- mRNA with no difficulties using the fluorescent antibody method, the enzyme immunoassay (ELISA) method, the radi- 40 oimmunoassay (RIA) method, the Western blot method and the immunostaining (immunohistochemistry) method. In the measurement of the expression level of the abnormal protein in step (f), the enzyme immunoassay (ELISA) method, the Western blot method, the immunostaining (immunohistochemistry) method and a mass spectrometry method can be used. [0090] In the measurement of the abnormal protein in step (f), an antibody against the abnormal protein generated 45 from the splicing defect of the genes listed Table 1, Table 2, Table 3, Table 4, and Table 5 and a fragment thereof can be used as a detection marker. [0091] Any abnormal protein may be employed for obtaining the antibody according to the present invention as long as it has antigenicity. A protein having an amino acid sequence of the abnormal protein wherein one or more amino acids are deleted, inserted, substituted or added can be used as the antigen for the abnormal protein. It is known that 50 such a protein maintains the same biological activity as the original protein (Mark et al. (1984) Proc.Natl.Acad.Sci.USA 81:5662-6; Zoller and Smith (1982) Nucleic Acids Res. 10:6487-500; Wang et al. (1984) Science 224:1431-3; Dalbadie- McFarland et al. (1982) Proc.Natl.Acad.Sci. USA 79:6409-13). A technique to delete, insert, substitute or add one or more amino acids while maintaining the antigenicity of the original protein is known. For example, such a protein may be obtained by preparing and properly expressing a polynucleotide encoding an abnormal protein by site directed 55 mutagenesis technique (Molecular Cloning, A Laboratory Manual 2nd ed., Cold Spring Harbor Press (1989); Current Protocols in Molecular Biology, John Wiley & Sons, (1987-1997), Section 8.1-8.5; Hashimoto-Goto et al. (1995) Gene 152:271-5; Kinkel (1985) Proc.Natl.Acad.Sci.USA 82:488-92; Kramer and Fritz (1987) Method.Enzymol. 154:350-67; Kunkel (1988) Method. Enzymol.85:2763-6).

14 EP 2 136 209 A1

[0092] The antibody according to the present invention includes an antibody having specificity against a part of the abnormal protein. That is, the abnormal protein for obtaining the antibody according to the present invention includes a polypeptide having the full length amino acid sequence of the abnormal protein as well as a fragment thereof having at least six amino acid residues (for example, not less than 6, 8, 10, 12 or 15 amino acid residues). A preferred fragment 5 is a polypeptide fragment such as an amino terminus and a carboxyl terminus of the abnormal protein. An antigen determination site of the polypeptide can be predicted by a method analyzing the hydrophobicity/hydrophilicity of the amino acid sequence of the protein (Kyte-Doolittle (1982) J.Mol.Biol. 157:105-22), and a method analyzing a secondary structure (Chou-Fasman (1978) Ann.Rev.Biochem. 47:251-76) and further confirmed by a computer program (Anal.Bi- ochem. 151:540-6 (1985)) or a technique such as PEPSCAN analysis (patent application publication JP60500684T) 10 involving the synthesis of a short peptide to confirm the antigenicity. [0093] Table 1, Table 2, Table 3, Table 4 and Table 5 describe information specifying the genes listed in these Tables and homologous genes thereof. Accordingly, those skilled in the art can obtain information on an amino acid encoded by the subject gene to be detected based on the information described in Table 1, Table 2, Table 3, Table 4 and Table 5, and can design and obtain an antibody based thereon. 15 [0094] In addition, the genes listed in Table 1, Table 2, Table 3, Table 4 and Table 5 are known genes and an antibody for detecting a protein encoded thereby is commercially available individually or as a detection kit or detection array. [0095] The antibody according to the present invention may be obtained with a method known those skilled in the art (for example, "Current Protocols in Molecular Biology" (John Wiley & Sons (1987), Antibodies: A Laboratory Manual, Ed. Harlow and David Lane, Cold Spring Harbor Laboratory (1988)). 20 [0096] The antibody according to the present invention includes a polyclonal antibody, a monoclonal antibody, a chimeric antibody, a single chain antibody (scFv), a humanized antibody and a multispecific antibody. Also, the fragment of the antibody according to the present invention includes an antibody fragment such as Fab, Fab’, F(ab’)2, Fc, and Fv. [0097] For a polyclonal antibody, blood can be taken from a mammal sensitized with an antigen and blood serum can be isolated with known procedures from the blood to yield blood serum containing the polyclonal antibody. As needed, 25 a fraction containing the polyclonal antibody can further be isolated from this blood serum. [0098] For a monoclonal antibody, antibody-producing cells are taken from spleen or lympho node of a mammal sensitized with the above-mentioned antigen, and then undergo cell fusion with myeloma cell. The resultant hybridoma is subjected to cloning and the antibody was recovered from the culture thereof to yield the monoclonal antibody. [0099] A fragment of the abnormal protein can be used as an immunogen. Alternatively, the synthesized one based 30 on the amino acid sequence of the abnormal protein can be used. The antigen can be used as a complex with a carrier protein. A variety of condensing agents can be used for preparation of the complex between the antigen and the carrier protein, which condensing agents include glutaraldehyde, carbodiimide, and maleimide active ester. The carrier protein may be a usually used one such as bovine serum albumin, thyroglobulin, and hemocyanin. A procedure for coupling at a rate (volume) of 1 time to 5 times is usually employed. 35 [0100] Examples of the animal immunized include mice, rats, rabbits, guinea pigs, hamsters. An example of a method of inoculation is subcutaneous, intramuscular or intraperitoneal administration. The administration may be done in com- bination with Freund’s complete adjuvant and Freund’s incomplete adjuvant, and usually once every two to five weeks. [0101] The antibody-producing cells obtained from the spleen or lymph node of the animal immunized undergo cell fusion with myeloma cells, and is isolated as hybridoma. As the myeloma cells, cells derived from mouse, rat, Homo 40 sapiens and etc. are used. It is preferred that antibody-producing cell be derived from the same species. Yet there are cases where the cell fusion can be carried out between different species. [0102] Procedures for the cell fusion may be carried out with a known method, in accordance with, for example, Nature, 256,495, 1975. Examples of fusion accelerator include polyethylene glycols and Sendai virus. The cell fusion can be usually carried out by using about 20 to 50% of concentration of polyethylene glycols (average molecular weight 1000 45 to 4000); at a temperature of 20 to 40°C, preferably 30 to 37°C; at a ratio in number of cells between antibody production cells and myeloma of usually about 1:1 to 10:1, and for about 1 to 10 minutes. [0103] Various immunochemical methods can be employed for screening the antibody-producing hybridoma. Exam- ples thereof include ELISA method using a microtiter plate coated with the abnormal protein, EIA method using a microtiter plate coated with an anti-immunoglobulin antibody, immune blot method using a nitrocellulose blotting membrane after 50 electrophoresis of samples containing the abnormal protein. [0104] Using such wells, cloning by, for example, a limiting dilution method can be further carried out to obtain a clone. Selection and breeding of the hybridoma is usually carried out culture medium for mammalian cells (such as RPMI1640) containing 10~20% bovine fetus serum and supplemented with HAT (hypoxanthine, aminopterin, and thymidine). The clone obtained in such a way is intraperitoneally transplanted into a SCID mouse previously administrated with pristine. 55 Ten to fourteen days later, ascites containing the monoclonal antibody at a high concentration is obtained, which ascites can be used as a raw material for antibody purification. Also the clone may be cultured and the obtained culture may be used as a raw material for antibody purification [0105] Any purification method may be used for purifying the monoclonal antibody as long as it is a known method

15 EP 2 136 209 A1

for purifying an immunoglobulin. The purification can be readily accomplished by, for example, an ammonium sulfate fractionation method, a PEG fractionation method, an ethanol fractionation method, and use of an anion exchanger, as well as means such as affinity chromatography using the abnormal protein. [0106] Purification of the polyclonal antibody from serum can be carried out in the same manner. 5 [0107] In cases where the procedure in the second aspect according to the present invention is carried out by using the cancer tissue and its surrounding tissue as assay samples, the action of the compound represented by formula (I) can preferably be assayed by using the expression level of the abnormal protein(s) expressed resulting from splicing defect of the genes listed in Table1 and Table 3 or homologous genes thereof as an index. In cases where the cancer tissue and the surrounding tissue are used as the samples, the measurement of the expression level of the abnormal 10 proteins can preferably be employed with the enzyme immunoassay (ELISA) method, the Western blot technique, the immunostaining (immunohistochemistry) method and the mass spectrometry method. [0108] In cases where the procedure in the second aspect of the present invention using peripheral blood or whole blood as assay samples, the action of the compound represented by formula (I) can preferably be assayed by using the expression level of the abnormal protein(s) expressed resulting from splicing defect of the genes listed in Table 2, Table 15 4, and Table 5 or homologous genes thereof as an index. In cases where peripheral blood or whole blood are used as the samples, the measurement of the expression level of the abnormal proteins can preferably be employed with the enzyme immunoassay (ELISA) method, the Western blot method, the immunostaining (immunohistochemistry) method and the mass spectrometry method. [0109] The samples obtained from a subject refer to tissues, cells, body fluids, and the like which are obtained from 20 the subject. Specific examples include biopsy, blood (including hemocytes, plasma, and serum), urine, tissue samples such as curettage tissue (buccal scrapes) of oral cavity, and tumor cells (cells from tumors of breast, lung, stomach, head and neck, colorectum, kidney, pancreas, uterus, liver, urinary bladder, endometrium, and prostate, as well as hemocytes of leukemia patients or of lymphocytes).

25 EXAMPLES

[0110] The present invention is described in more detail by the examples below. The followings are illustrative of the invention and by no means intended to limit the invention to the embodiments described herein.

30 Example 1: Analysis with Northern blotting

[0111] Gene expression that affects the cell cycle was examined by Northern blotting analysis using RNA from HeLa cells treated with pladienolide B. As a result, it was discovered that CDKN1B (p27) gene caused pre-mRNA accumulation. [0112] HeLa cells (5x105 cells/mL) were first seeded in a six-well plate and cultured overnight in RPMI1640 medium 35 (containing 10% FCS, penicillin, and streptomycin). The cells were then treated with 10 PM of pladienolide B, 100 PM of DRB, or 1Pg/mL of Actinomycin D for 0, 1, 2, and 4 hours. Subsequently, total RNA was obtained using RNeay mini kit (Qiagen) and absorbance at 260 nm was measured to quantify an amount of RNA. Each total RNA sample (10 Pg) was, after combined with RNA SAMPLE LOADING BUFFER (SIGMA), subjected to electrophoresis in 1% denatured agarose gel containing formaldehyde, followed by blotting to nylon membrane and cross-linking with UV to make a 40 Northern membrane. [0113] In order to make a probe for CDKN1B(p27) and CDKN1A(p21), the entire length of gene was amplified by PCR with the following primers using cDNA reverse-transcribed from total RNA prepared from U251 cells as a template.

Primers for CDKN1B 45 [0114]

P27-1F: 5’-ATGTCAAACGTGCGAGTGTCTAAC-3’ (SEQ ID NO: 1) P27-2: 5’-TTACGTTTGACGTGTTGTGAGGCC-3’ (SEQ ID NO: 2) 50 Primers for CDKN1A

[0115]

55 P21-1F: 5’-GCCATGTCAGAACCGGCTGGGGAT-3’ (SEQ ID NO: 3) P21-2: 5’-TTAGGGCTTCCTCTTGGAGAAGAT-3’ (SEQ ID NO: 4)

The obtained fragment was separated by electrophoresis in agarose gel and purified. The fragment was labeled using

16 EP 2 136 209 A1

Megaprime DNA labeling kit (Amersham) and Redivue 32P (Amersham) and purified with ProbeQuant G-50 Micro Col- umns (Amersham). Using PerfectHyb hybridization solution (TOYOBO), the labeled probe was hybridized onto the blotting membrane. The membrane was washed with a buffer containing 2xSSC and 0.05% SDS, followed by a buffer containing 0.1SSC and 0.1% SDS. The membrane was exposed to Imaging Plate (FUJIFILM) to determine intensity 5 of photosensitivity with BAS2000 (FUJIFILM). Accumulation of CDKN1B pre-mRNA was observed only when the cells were treated with pladienolide (Figure 1A and B).

Example 2: Analysis with cDNA library

10 [0116] In order to check if any other gene accumulated its pre-mRNA, a cDNA library was constructed from HeLa cells treated with pladienolide and by randomly sequencing 42 clones, genes containing an intron were screened. Primers were designed within the introns surrounding an exon of those genes. RT-PCR was performed for the total RNA of HeLa cells treated with pladienolide. DNAJB1, BZW1, SPAG5, RIOK3, NUP54, and BRD2 were identified as pre-mRNA- accumulating genes. 15 [0117] Semi-confluent HeLa cells cultured in a 10 cm dish in DMEM high glucose medium (containing 10%FCS, penicillin, and streptomycin) were treated with 10nM, 100nM, and 10PM of pladienolide B for 4 hours and 6 mL of TRIzol (Invitrogen) was added thereto so that the cells were dissolved. Total RNA was obtained in accordance with the protocol of TRIzol and absorbance at 260 nm was measured to quantify an amount of RNA. [0118] Subsequently, mRNA was purified from total RNA collected from HeLa cells treated with 10nM, 100nM, 10P 20 of pladienolide B and without the treatment, using PMACS mRNA Isolation Kit (Miltenyi Biotec). mRNA was concentrated by ethanol precipitation and absorbance at 260 nm was measured to quantify an amount of RNA. For 1Pg of mRNA, single stranded cDNA synthesis, double stranded cDNA synthesis, adaptor ligation in order was carried out using SuperScript Plasmid System for cDNA Synthesis and Cloning (Invitrogen), and the resultant DNA fragment was ligated to pCLex, which is a retovirus vector. The resultant vector construct was then transformed into XL10-Gold ultracompetent 25 cells (STRATAGENE). The transformed cells were seeded on LB plates containing ampicillin and cultured overnight. From each plate of the sample treated with 10nM, 100nM, and 10PM of pladienolide B and without the treatment, 42 clones were separately picked up. A total of 42 clones was individually cultured and the plasmid was purified. [0119] A nucleotide sequence of the genes inserted in the plasmid of the 42 clones extracted from the cDNA library of the sample treated with 10nM, 100nM, and 10PM of pladienolide B and without the treatment was obtained using 30 BigDye Terminator(Applied Biosystems) and senseXIY primer (sequence: CCTCGATCCTCCCTTTATCCAGCCCT- CACT) (SEQ ID NO: 5) with ABI PRISM3130 (Applied Biosystems). The obtained sequence was then compared with genome information with UCSC/BLAT to collect genes containing a sequence of an intron region. For the genes containing the sequence of the intron region, the following primers were designed within both-sided exon regions surrounding the intron region. 35 DNAJB1-FW:

[0120]

40 5’-GAACCAAAATCACTTTCCCCAAGGAAGGAG-3’ (SEQ ID NO: 6)

DNAJB1-RV:

[0121] 45 5’-AATGAGGTCCCCACGTTTCTCGGGTGT-3’ (SEQ ID NO: 7) BZW1-FW: 5’-GCCAATAAGCAAAGTGTTGAACACTTCAC-3’ (SEQ ID NO: 8)

BZW1-RV: 50 [0122]

5’-AAGTGCTTGATGGCTTGCTCTGCTAC-3’ (SEQ ID NO: 9)

55 SPAG5-FW:

[0123]

17 EP 2 136 209 A1

5’-ACATGGACAGCTTTGCTGAGTCGGTCC-3’ (SEQ ID NO: 10)

SPAG5-RV:

5 [0124]

5’-TTGCTAGACGACTGTTTfCCAACTCCAG-3’ (SEQ ID NO: 11)

RIOK3-FW: 10 [0125]

5’-GCTGAAGGACCATTTATTACTGGAG-3’ (SEQ ID NO: 12) RIOK3-RV: 5’-TTCTTGCTGTGTTCTTTCTCCCACA-3’ (SEQ ID NO: 13) 15 NUP54-FW:

[0126]

20 5’-CTAATCAAACAGGAAATTCAAAGGAAGAG-3’ (SEQ ID NO: 14)

NUP54-RV:

[0127] 25 5’-CTTGATTTCTCGTAACAGATCTGCATC-3’ (SEQ ID NO: 15)

BRD2-FW:

30 [0128]

5’-ACTCTCAGCAACAACACCAGAGCTCTA-3’ (SEQ ID NO: 16)

BRD2-RV: 35 [0129]

5’-TAGCTTTCGTGCCATTGCCACAACATC-3’ (SEQ ID NO: 17)

40 Total RNA was collected from HeLa cells treated with 100nM or 1PM of Pladienolide B for 1, 2, or 4 hours or untreated. The total RNA was treated with DNase, and then subjected to reverse transcription reaction to yield cDNA. The obtained cDNA was then subjected to PCR using FastStart HiFi Polymerase (Roche Diagnostics) with the designed primers. Based on an electrophoresis pattern in agarose gel, a decrease in the expression of mature RNA and an increase in the expression of premature mRNA upon the Pladienolide B treatment was confirmed in DNAJB1, BZW1, SPAG5, 45 RIOK3, NUP54, and BRD2 (Figure 2).

Example 3: Analysis with microarray

[0130] Using RNA purified from human colon carcinoma cell strain WiDr treated with 14 nM of (8E,12E,14E)-7-((4- 50 cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytric osa- 8,12,14-trien-11-olide (also referred to as "E7101") for six hours, microarray analysis (Human Exon 1.0 ST Array: Af- fymetrix) was carried out. Not only does this array comprehensively cover the exons for all genes, but it is also designed to have probes for regions estimated as potential exons by a computer prediction program, which enables detection of the expression of the exons and introns of all genes in theory. As a result, genes of which mature mRNA was sufficiently 55 expressed when untreated and of which intron exhibited not less than ten times increase upon the treatment with (8E, 12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19- epoxytric osa-8,12,14-trien-11-olide in at least two probe sets were identified. [0131] WiDr cells were first suspended in RPMI1640 medium (containing 10% FBS, penicillin, and streptomycin) and

18 EP 2 136 209 A1

seeded in a 10 cm dish (2x106 cells/dish). After an overnight culture in an incubator with 5% carbon dioxide gas at 37°C, the medium was changed with medium containing 14 nM of (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy- 3,6, 16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytric osa-8,12,14-trien-11-olide or containing vehicle alone. After cultured for additional six hours, TRI reagent (SIGMA) were added to the cells and the cells were harvested. 5 RNA was purified in accordance with the protocol of TRI reagent, followed by further purification with RNeasy (QIAGEN). Absorbance at 260 nm was measured to quantify an amount of RNA. This experiment was repeated three times and RNA samples (n=3) were prepared. [0132] Ribosomal RNA was removed from 1 Pg of each total RNA of control cells (n=3) and cells with the treatment (n=3) by using RiboMinus Human/Mouse Transcriptome Isolation Kit (Invitrogen). Single stranded cDNA synthesis, 10 double stranded cDNA synthesis, cRNA synthesis, second single stranded cDNA synthesis, cDNA fragmentation, and cDNA labeling in order were carried out for the total RNA from which ribosomal RNA was removed, by using GeneChip Whole Transcript Sense Target Labeling and Control Reagents (Affymetrix) to make a cDNA probe. The cDNA probe was used for hybridization with Human Exon 1.0 ST Array (Affymetrix). The array was washed and stained, and luminescence intensity was measured by a scanner. 15 [0133] The expression level of the probe set and the gene was quantified by using Expression Console Ver. 1.0 (Affymetrix) with Summarization Method and Normalization Method being set to "Median polish as used in RMA" and "None", respectively. The expression level of the probe was normalized with that of the gene. Welch’s t-test was conducted for the treated group and the control group to determine a p value, which was converted into a q value by controlling False Discovery Ratio to pick out a significant probe set. 20 [0134] Probe sets showing that the q value was less than 1%; the normalized change in the level expression of the probe set in the group with the treatment was more than 10 times; the expression level of the probe set and the gene in the group with the treatment was more than 100; and probe set annotation was "extended, full, free", were picked out and further arranged by gene. A gene was, when more than one probe sets therefor were found, determined as a candidate gene with increased expression level of the intron regions (Table 1). In Table 1, for the gene evaluated, gene 25 name (Gene Name), abbreviated name (Gene Symbol), accession number (Accession), alias name (Synonym), transcription number in Human Exon 1.0 ST Array (Human Exon 1.0 ST Array), chromosome number (Chromosome), type of strand (Strand), start region (Start), stop region (Stop), and change in expression level (Fold Change) were respectively shown.

19 EP 2 136 209 A1 Fold Fold Change

15 Human Genome hg18 Genome Human

20 Chromosome Strand Start Stop

25 Human 3497586 chr13 +2468811 96672563 chr2 96644371 28.86 3284188 + chr10 9264345 9463243 - 22.92 332110513233322 33321367 21.48 chr10 + 5766851 5846629 19.86 2556752 chr2 - 65391279 65513247 31.56 Exon 1.0 1.0 Exon ST Array

30 [Table 1] [Table alpha // alpha 2

35 DKFZp781H1296 // MBLL // // MBLL // DKFZp781H1296 // MGC120625 // MBLL39 // MGC120828 // MGC120828 PRO2032 // FLJ20360 // DKFZp781E1986 bA318E3.2 AMAP2 // FLJ42910 // KIAA0400 KIAA0400 // // FLJ42910 AMAP2 // Pap- // PAP // PAG3 SHAG1 // // MDF2 // GPDA CD29 // FNRB VLAB // MSK12 40 // // FLJ31917 FLJ21897 Spred- // MGC163164 144778 // 144778 207304 018321 FLJ11100 // BRIX 003887 // 002211 // 033867 2806231 // 033668 033669 chr5 012154 + Q10 // // MGC3183 AGO2 34951248 34962845 3156193 25.94 014761 MGC117220 chr8 - 141599440 141726037 3667766 21.33 chr16 + 70481983 70522196 19.65 032856// HSPC264 FLJ1488B 3636956 chr15 - 82987018 82998719 30.61 181784 374765

45 Accession Synonym NM_ NM_ NM_ NM_ NM_ NM_ Gene Gene ITGB1 DDEF2 NM_ BXDC2 NM_ Symbol MBNL2 EIF2C2 NM_ WDR73 NM_ SPRED2 NM_ 50 C10orf18 XM_ like 2 like

55 related, related, Gene Name brix domain domain brix 2 containing development and differentiation 2 factor enhancing 1 beta integrin, (fibronectin beta receptor, polypeptide, CD29 antigen MDF2, includes MSK12) eukaryotic initiation translation 2 2C, factor chromosome 10 frame reading open 18 K1AA0174 KIAA0174 NM_ WD repeat domain domain repeat WD 73 muscleblind- (Drosophila) sprouty- domain EVH1 2 containing

20 EP 2 136 209 A1 Fold Fold Change

15 Human Genome hg18 Genome Human

20 Chromosome Strand Start Stop

25 Human 3614087 chr15 - 23006655 23355108 19.35 2542816 chr2 -3240340 20291440 20450197 chr102929038 19.01 chr62333136 + 28828043 chr1 + 29005095 18.53 144194149 + 144227146 18.37 43597180 43601431 18.22 Exon 1.0 1.0 Exon ST Array

30 (continued) AP // EPVE6AP

35 1 // ILF1 1 3738969 chr17 + 78070883 78195807 18.79 016 // MGC10753 // PRO1741 // PRO1741 // MGC10753 016 ANCR // AS E6- HPVE8A // // FLJ28981 // // KIAA0235 FLJ38528 // 38253 MGC1 // MGC138251 // PUML2 PUMH2 BM- // bA48B24.1 // bA48B24 // Wwp4 // // FLJ14909 C6orf93 dJ468K18.4 40 // // MGC102824 CDC20A // p55CDC bA276H19.3 000482 // 000482 // 130838 130839 015317 003171 SUV3 004514 // 016828 // ILF- ILF // 100284 100486 032860 3250204 chr10 + 70609946 70638996 18.81 080927// ESDN CLCP1 2686023 004508 chr3// IPPI1 IPP1 018064 // dJ488L4.2 FLJ10342 - 99997526 100124598 2963784 3273601 19.52 chr10 chr6 - - 88441297 1075869 88476721 1092634 001255 19.23 19.25

45 Accession Synonym NM_ NM_ NM_ NM_ NM_ NM_ IDI1 NM_ WAC LTV1 NM_ Gene Gene PUM2 NM_ UBE3A CDC20 NM_ Symbol DCBLD2 NM_ C6orf166 NM_

50 SUPV3L1 NM_ roil 55 Gene Name like 1 (S. 1 like forkhead box K2 box forkhead FOXK2 NM_ WW domain domain WW adaptor containing coiled- with associated protein. protein. associated Angelman syndrome) discoidin, CUB and and CUB discoidin, domainLCCL 2 containing protein ubiquitin E3A (human ligase E6- virus papilloma isopentenyl- chromosome 6 frame reading open 166 2 homolog pumilio (Drosophila) var1, of suppressor 3- cerevisiae) (S. homolog LTV1 cerevisiae) CDC20 cell division 20 homolog cycle cerevisiae) (S. diphosphate delta delta diphosphate 1 isomerase

21 EP 2 136 209 A1 Fold Fold Change

15 Human Genome hg18 Genome Human

20 Chromosome Strand Start Stop

25 Human 29819123398402 chr6 chr11 - - 159106770 159160432 130250320 17.50 1302918152409104 17.12 chr1 - 43124794 43338329 16.44 Exon 1.0 1.0 Exon ST Array

30 (continued) Raf 2663244 chr3 - 12600117 12680654 16.41

35 // EIF4A 4A 3708826 chr17 + 7416768 7423040 16.15 1 // c- 1 43 2320048 chr1 + 10995025 11013170 18.13 FAC1 // FALZ // NURF301 // // FALZ FAC1 3732448 chr17 + 63252111 63410954 // // MGC141885 // GLUT1 GLUT 17.61 MGC141896 40 // // DKFZp762H157 CVL CVIL // MGC1584 // FW26216 // DKFZp6671205 // CHET8 KIAA0254 022490Raf- CRAF // 013242GTL3 // EVORF 001418 EIF- // DDX2A 3693511 chr16 - 56683698 56739201 16.25 007375 TDP- // 004459 182641 006516 003379 014758 138375 // HsT2563 FLJ35924 022739// MGC138150 DKFZp888F0270 3786960 3761531 chr17 chr18 - + 59968891 18940699 60088896 19101598 16.60 16.94

45 Accession Synonym NM_ NM_ Gene Gene RAF1 NM_ BPTF Symbol E1F4A1 NM_ SLC2A1 NM_ TARDBP NM_ C16orf80 NM_ SMURF2 NM_

50 CABLES1 NM_

55 1 murine Gene Name raf- leukemia viral viral leukemia homolog oncogene 1 chromosome 16 frame reading open 80 eukaryotic initiation translation 1 isoform 4A, factor fetal Alzheimer Alzheimer fetal antigen TAR DNA binding TAR DNA protein 2 (ezrin)villin 19 nexin sorting VIL2Cdk5 and Ab1 1 substrate SNX19enzyme NM_ E3 specific SMAD NM_ protein ubiquitin 2 ligase solute carrier family 2 (facilitated glucose transporter), member 1 v-

22 EP 2 136 209 A1 Fold Fold Change

15 Human Genome hg18 Genome Human

20 Chromosome Strand Start Stop

25 Human 3508330 chr13 - 30558258 30851892 15.12 36288263494137 chr15 chr13 +3145020 57215720 57452363 75092571 14.49 chr82444451 75566974 14.34 4009062 chr1 - chrX 95569109 - 95834851 172035313 14.19 - 172104622 14.13 53159032 53271329 14.09 3020192 chr73050535 chr16 +3470253 115637811 + 115743800 chr12 15.95 30081120 - 30695182 15.84 107440140 107479296 15.13 Exon 1.0 1.0 Exon ST Array 30 (continued) 25 L // FLJ31044 FLJ31044 // L CO- 35 // TESTIN 2 10 // MGC104638 // // MGC104638 10 HuncM- MYO1C // DKFZP434I118 MGC138493 // DKFZp781B2117 // MSTP054 // MGC141940 FBX20 // FBXO20 // KIAA0858 // // KIAA0858 FBXO20 // FBX20 LOMP CENP- // 55 orf1 C1 dJ383J4.3 // // RP3-383J4.1 // MRXSJ // MRXJ // DXS1272E // XE169 SMCX KIAA0156 // MGC138188 // // MGC138188 KIAA0156 p110 // // TIP110 RP11-13G14 (nrb) 40 // MGC1146 // DKFZP586B2022 TESS- TESS II // DKFZp686K191 BRE1B // RBP95 // MGC13051 // KIAA0661 // STARING // HSP105 // DKFZp688M05240 // HSP1058 // HSP105A // NY- KIAA0201 025010 // KIAA0795 FLJ13703 004998 2621275 chr3 183009 + 47298888 47387590 15.00 005358 133388 KIAA1972 033319 004187 3662612 chr16 + 55777703 55831882 14.32 014706 014771 006644

45 Accession Synonym NM_ 015641//NM_ 152829 0154986// 0154986// NM_ NM_ TES Gene Gene RNF40 NM_ Symbol CENPL NM_ HSPH1 NM_ KLHL18 NM_ START3 NM_ RSPRY1 NM_ 50 JARID1C NM_

55 like 18 Gene Name testis derived LIM (3 transcript domains) kelch- (Drosophila) myosin 1E MYO1E NM_ UM domain 7 domain UM and finger ring SPRY domain 1 LMO7containing NM_ KIAA1429 protein centromere L KIAA1429 X- homolog, Smcy (mouse) linked ring finger protein protein finger ring 40 cell squamous antigen carcinoma recognised by T coils 3 105kDa/ shock heat 1 proteins 110kDa

23 EP 2 136 209 A1 Fold Fold Change

15 Human Genome hg18 Genome Human

20 Chromosome Strand Start Stop

25 Human 2877508 chr5 - 137917364 137939144 13.33 3598959 chr15 + 65145043 65296818 12.88 3194635 chr9 + 136810077 138855460 13.66 Exon 1.0 1.0 Exon ST Array

30 2 (continued) PARF// PARF//

35 DKFZp779L1370 // SUDD DKFZp779L1370 3781654 chr18 + 19161035 19320545 13.87 DKFZP586N0721 // DKFZP586N0721 // // HSPC193 DKFZ686J10186 // // MADH3 JV15-2 // HsT17438 MGC60396 //Smad 3 FLJ10101 // FLJ13045 // Parf // // Parf // FLJ13045 FLJ10101 // bA218L13.9 // RP11-216L13.9 MGC15438// // pp8875 RP11-216L13.7//RP11-216L13.9 // bA216L13.7 40 NS // MGC800 // E2IG3 // C77032 2624074 chr3 + 52694976 52705212 14.08 HSPA9B // // GRP75 CSA // // MOT2 // // MOT MGC4500 mot- // // PBP74 MTHSP75 003831 // 003831 145808 // 024718 004515 PRO3063 // // NF45 MGC8391 2436132 chr1 - 151900372 151910103 13.79 002130 MGC90332 // HMGCS 005603 NET1A // ARHGEF8 2855501 005902 chr5 3233182 - chr10 43324231 + 43349337 13.21 5444535 5491001 13.02 014388 // 014388 206825 007002// Rpn13 // MGC29536 GP110 000224 // K18 CYK18 3892607 004134 chr20 + 3415576 60305485 60317305 chr12 13.51 + 51596769 51632949 13.41

45 Accession Synonym NM_ NM_ 001039374 NM_ NM_ NM_ NM_ ILF2 NM_ Gene Gene NET1 NM_ GNL3 RIOK3 HSPA9 NM_ Symbol SMAD3 NM_ ADRM1 NM_ HMGCS1 NM_ 50 // C9orf86 KLAA1984 like like 3- 55 Gene Name hydroxy- interleukin interleukin binding enhancer 45kDa 2, factor chromosome 9 frame reading open KIAA1984 // 86 3- mothylglutaryl- Coenzyme A 1 (soluble) synthase cell neuroepithelial transforming gene 1 mothers SMAD, DPP against 3 homolog (Drosophila) adhesion regulating 1 molecule 18keratin 70kDa shock heat 98 (mortalin- protein 2) KRT18 NM_ RIO kinase 3 kinase RIO (yeast) 3 (nucleolar) guanine nucleotide nucleotide guanine proteinbinding

24 EP 2 136 209 A1 Fold Fold Change

15 Human Genome hg18 Genome Human

20 Chromosome Strand Start Stop

25 Human 3154398 chr83338192 - chr11 134535811 134653449 12.77 + 69161881 69170408 12.66 4041923 chr1_random + 359569 372958 12.84 3320604 chr11 + 118195563319937 11937446 1232 3231774 chr11 chr10 + + 9550916 9579143 942450 12.26 1055862 12.24 Exon 1.0 1.0 Exon ST Array

30 ISO // // ISO (continued)

35 // ST30 1 6B // DKFZp761A1210 // // DKFZp761A1210 6B 3 // WIPI3 3 // 3775157 chr17 - 78165748 78199803 12.59 ISO // PCEE // S8138 PCEE // ISO // 5A 3553607 chr14 + 102743652 102881108 12.30 NAc6S // MGC8183 // SIAT4A // SIAT4A MGC8183 // NAc6S BCL1 // D11S287E // PRAD1 // // PRAD1 // // D11S287E BCL1 U21B31 KIAA0410 // PRO2463KIAA0410 3482219 chr13 + 24773258 24622202 12.63 Gal- // ST3GalA. ST3GalA // // SIATFL 1 // ST3GalIA. // // FLJ20727 DKFZp6876C3257 TRFP // FLJ16446 // DKFZp686118166 WEE1hu CRFG // FLJ10686 // FLJ10690 // // FLJ10690 // FLJ10686 // CRFG // NGB FLJ39774 40 ANIA- HCLA- // DKFZp7620195 HLA- 014089 // 014089 018093 // FLJ21730 FLJ10439 053056 3376235 chr11 - 62356627 62365857 12.70 003033 019613 WIPI- 017944 001969 EIF- 005911 SAMS2 // MATII // MATA2 003390 2491615 chr2 + 85597809 85625908 12.29 012341 030937

45 Accession Synonym NM_ // 001008564 NM 001008565 NM_ E1F5 NM_ Gene Gene WEE1 NM_ USP47 NM_ Symbol MAT2A NM_ WDR74 NM_ GTPBP4 NM_

50 ST3GAL1 NM_

55 like WDR45L NM_ Gene Name WD repeat domain domain repeat WD 74 cyclin D1 1 like nucleoporin CCND1 NUPL1 NM_ ST3 bata- ST3 WDR45- (S. homolog WEE1 pombe) galactoside alpha- galactoside 2,3- 1 sialyltransferase ubiquitin specific specific ubiquitin 47 peptidase methionine adenosyltransferas e II. alpha eukaryotic eukaryotic initiation translation 5 factor protein binding GTP 4 cyclin L2 CCNL2 NM_

25 EP 2 136 209 A1 Fold Fold Change

15 Human Genome hg18 Genome Human

20 Chromosome Strand Start Stop

25 Human 3615579 chr15 - 27703228 28048334 11.55 3996667 chrX ++ 153644243 153659150 11.53 3283920 chr10 - 32134245 32261226 11.60 3442205 chr12 - 6645924 6668961 12.13 2891052 chr5 - 180596592 180612024 11.87 Exon 1.0 1.0 Exon ST Array

30 7 // 7 (continued)

35 iso // XTP2 // iso 2367154 chr1 + 169716078 169829202 11.26 rs1 // H12.3 // HLC- // H12.3 rs1 1 1 // APA1 3543884 chr14 + 73423093 73468718 12.01 DKC // NAP57 // NOLA4 // XAP101 XAP101 // NOLA4 // NAP57 DKC // // dyskerin DKFZp686M05161// MCC133289 MCC133289 DKFZp686M05161// // ZO- DKFZp779N2050 // FLJ10971 // FLJ10971 // DKFZp779N2050 // // FLJ21785 FLJ20737 FLJ45709 CAGH1 // CAGH1A // CIZ // // CIZ CAGH1A // CAGH1 // TNRC1 // NP NMP4 ERDA2 // Gnb2- // RACK1 PIG21 40 // MQC1798ATP1B 2366422 chr1 + 167342204 167368946 12.11 001363 015172 BAT2- 003257 // 003257 175610 018287 001677 // 001677 133476 006098 012402 POR1 021188 APA- 006145 Hsp40 // // Hdj1 HSPF1 3360941 3852783 chr11 chr19 - - 14485622 6453496 14501114 6439171 11.95 12.04

45 Accession Synonym NM_ NM_ NM_ NM_ 001001787 NM_ 2 TJP1 Gene Gene DKC1 NM_ Symbol ARFIP2 NM_ ZNF384 NM_ ZNF410 NM_ ATP1B1 BAT2D1 NM_ GNB2L1 NM_ 50 DNAJB1 NM_ ARHGAP1

+ like 1 like

55 ribosylation ribosylation Gene Name dyskeratosis dyskeratosis 1, congenita dyskerin BAT2 domain domain BAT2 1 containing tight junction junction tight (zona 1 protein 1) occludens zinc finger protein protein finger zinc 384 Na+/K ATPase, zinc finger protein protein finger zinc 410 nucleotide guanine (G protein binding beta protein), 2- polypeptide GTPase Rho protein activating 12 DnaJ (Hsp40) subfamily homolog, B. member 1 ADP- interacting factor 2) 2 (arfaptin protein transporting, beta 1 beta transporting, polypeptide

26 EP 2 136 209 A1 Fold Fold Change

15 Human Genome hg18 Genome Human

20 Chromosome Strand Start Stop

25 Human Exon 1.0 1.0 Exon ST Array

30 B 2772017 chr4 - 68858700 68934802 10.66 (continued)

35 ADK2 2405364 chr1 - 33245959 33275155 10.05 40 // YT521- // YT521 KIAA1986 001625 // 001625 013411 012461 TIN2 3558012 chr14 - 23776465 23781950 11.05

45 Accession Synonym NM_ NM_ NM_ 001031732 Gene Gene TINF2 NM_ Symbol 50 YTHDC1

55 Gene Name YTH domain 1 containing 2kinase adenylate AK2 TERF1 TERF1 (TRF1)-interacting 2 factor nuclear

27 EP 2 136 209 A1

Example 4: Analysis in PBMC

[0135] Since it is not easy to obtain a cancer tissue clinically, the measurement of the marker in hemocytes readily obtainable in peripheral blood would be more useful. It was then examined whether the marker gene obtained in cancer 5 cells could change in peripheral blood mononuclear cells in a similar manner as observed in the cancer cells. Specifically peripheral blood was taken from three normal individuals (volunteers) and peripheral blood mononuclear cells were purified and treated with (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy- 6,10,12,16,20-pentamethyl-18,19-epoxytric osa-8,12,14-trien-11-olide for three hours, followed by measurement of change in expression of the precursor gene (pre-mRNA) by qPCR. In cases where an increase in the expression of pre- 10 mRNA is used as a marker, the genes in Table 2 below, as a representative example, were found to be usable.

(1) Isolation of peripheral blood mononuclear cells (PBMC)

[0136] Ficoll-Paque PLUS solution (Amersham, 17-1440-02) was slowly added to the blood taken (with heparin added) 15 from healthy individuals to form a layer underneath the blood (15 mL of Ficoll-Paque PLUS solution was added to 25 mL of blood). After the mixture was centrifuged at 1500 rpm for 30 min, the upper part containing platelets was removed and then a layer containing mononuclear cells was transferred to another tube. The cells were suspended in PBS and centrifuged at 1500 rpm for 5 min, followed by removal of the supernatant. After these steps were repeated twice, the PBMC was suspended in RPMI1640 (containing 10% FBS, penicillin, and streptomycin) and the number of the cells 20 was then counted.

(2) Preparation of total RNA

[0137] PBMC was suspended in RPMI1640 medium (containing10% FBS, penicillin, and streptomycin) to 5x106 25 cells/ml and 1 ml of the suspension was plated per well of a 24-well plate. Immediately, 111 Pl of 10 times-concentrated (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19- epoxytric osa-8,12,14-trien-11-olide was added to the well (six wells per each concentration tested). The cells were then cultured in an incubator with 5% carbon dioxide gas at 37°C. Three hours later, the supernatant was collected and centrifuged at 1500 rpm for five minutes. TRI reagent (SIGMA) (1 ml) was added to each well of the plate from which 30 the supernatant was removed to harvest the cells, which was added to the centrifuged pellet to dissolve. RNA was purified in accordance with the protocol of TRI reagent. RNA was further purified using RNeasy (QIAGEN) and, in accordance with the protocol, DNaseI was added to the samples during the procedure. Absorbance at 260 nm was measured to quantify an amount of RNA.

35 (3) Measurement of the expression level of a precursor gene (pre-mRNA)

[0138] RNA was prepared to 30 ng/Pl and cDNA was synthesized using TaqMan Reverse Transcription Reagents (Applied Biosystems). For the expression level of pre-mRNA of ID1, amplification was carried out by using TaqMan Universal PCR Master Mix (Applied Biosystems) with TaqMan Gene Expression Assays (Hs00704053_s1 Applied Bi- 40 osystems) as a probe. For the expression level of pre-mRNA of DNAJB1, BZW1, NUP54, RIOK3, CDKN1B, STK17B, ADRM1, EIF4A1, FOXK2, GNB2L1, HSPA9B, HSPH1, KLHL18 and VIL2, reagents were prepared in accordance with each protocol by using POWER SYBR GREEN PCR MASTER MIX (Applied Biosystems) and primers with the sequence below (Invitrogen), and the expression level was measured with ABI7900 (Applied Biosystems). 18S rRNA was measured by both the TaqMan and SYBR methods. The expression level of 18S r RNA was measured with Hs99999901_s1 45 (Applied Biosystems) as primers for TaqMan and with 18S primers included in TaqMan Ribosomal RNA control reagents (4308329: Applied Biosystems) as primers for SYBR. Measured values were corrected using the expression level of 18S rRNA as an internal control. The expression level of each gene was calculated with the expression level in the cells treated without (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytric osa-8,12,14-trien-11-olide as 1. Genes of which expression level in PBMC reached about 50 250% or more were shown in Table 2.

DNAJB1:

[0139] 55 Sense: 5’-GGCCTGATGGGTCTTATCTATGG-3’ (SEQ ID NO: 18) Antisense: 5’-TTAGATGGAAGCTGGCTCAAGAG-3’ (SEQ ID NO: 19)

28 EP 2 136 209 A1

BZW1:

[0140]

5 Sense: 5’-GAACTTTGCCTCATTCTTTTGCA-3’ (SEQ ID NO: 20) Antisense: 5’-CTGAGCTCCAGTCTCTTGTATTTCTG-3’ (SEQ ID NO: 21)

NUP54:

10 [0141]

Sense: 5’-CAAGGTAACCACTTCTAAGACCATAATTC-3’ (SEQ ID NO: 22) Antisense: 5’-CCTGCTTGAAGATTACATAACTTTTTGT-3’ (SEQ ID NO: 23)

15 RIOK3:

[0142]

Sense: 5’-TCAATGGAGATAGCAAAGGTATTATAACC-3’ (SEQ ID NO: 24) 20 Antisense: 5’-AGATTTACTTAGGAGCACATTATGAGTGTT-3’ (SEQ ID NO: 25)

CDKN1B (p27):

[0143] 25 Sense: 5’-ATGTTTATCAACGGTCCGCCT-3’ (SEQ ID NO: 26) Antisense: 5’-CATCCCCAGTGGCTTTTAAGG-3’ (SEQ ID NO: 27)

STK17B: 30 [0144]

Sense: 5’-TGCGCGGAGACAGCATAG-3’ (SEQ ID NO: 28) Antisense: 5’-TGGGTTCAAAATGCCAGGTT-3’ (SEQ ID NO: 29) 35 ADRM1:

[0145]

40 Sense: 5’-GGCCCTTCAGAAATGCTTGTC-3’ (SEQ ID NO: 30) Antisense: 5’-CCCATTACACAATTCATGTGCTTAG-3’ (SEQ ID NO: 31)

EIF4A1:

45 [0146]

Sense: 5’-CAGATCATCTAGAAGCAGCTGGTTT-3’ (SEQ ID NO: 32) Antisense: 5’-ACAGAATCTGGTGCCTACTAACAAAA-3’ (SEQ ID NO: 33)

50 FOXK2:

[0147]

Sense: 5’-GAGCAGAAGGAAGCGTGGTT-3’ (SEQ ID NO: 34) 55 Antisense: 5’-GACACATGAATTTCCACAACAGTAAA-3’ (SEQ ID NO: 35)

29 EP 2 136 209 A1

GNB2L1:

[0148]

5 Sense: 5’-ACGTAATGACATTTTGGTCTGAGTAACT-3’ (SEQ ID NO: 36) Antisense: 5’-AAATGCTGCTAAACATCCTGGAA-3’ (SEQ ID NO: 37)

HSPA9B:

10 [0149]

Sense: 5’-TGAATCCTGAATACTATGCCTCCTT-3’ (SEQ ID NO: 38) Antisense: 5’-TCCCTTCTTCTCAAGACTACTCAGTATG-3’ (SEQ ID NO: 39)

15 HSPH1:

[0150]

Sense: 5’-ACCTTCTTCTCACAAGACTTTTTAAGC-3’ (SEQ ID NO: 40) 20 Antisense: 5’-CCTTCTCAGCCACCATGGAA-3’ (SEQ ID NO: 41)

KLHL18:

[0151] 25 Sense: 5’-CCAGGTTTCCCCTGCAGTT-3’ (SEQ ID NO: 42) Antisense: 5’-CCCCCTGACTTAGTCCTCGTT-3’ (SEQ ID NO: 43)

VIL2: 30 [0152]

Sense: 5’-CCCACTGCCTTGATCTAGTTGAT-3’ (SEQ ID NO: 44) Antisense: 5’-GTCAAGCAATCTATGGCCTACCA-3’ (SEQ ID NO: 45) 35 In Table 2, for the gene evaluated, abbreviated name (Gene Symbol), accession number (Accession), alias name (Synonym), gene name (Gene Name), chromosome number (Chromosome), type of strand (Strand), start region (Start), stop region (Stop), and the expression level at 0 hours, three hours, 10 hours and 30 hours after the E7107 treatment were respectively shown. 40 [Table 2] E7107 (nM) Gene Symbol Accession Synonym Gene Name 0 3 10 30 45 DnaJ (Hsp40) HSPF1 // Hdj1 // DNAJB1 NM_006145 homolog, subfamily 1 2.25 4.46 7.42 Hsp40 B, member 1 BZAP45 // XM_001126385 // basic leucine zipper BZW1 KIAA0005 // 1 1.72 2.34 3.26 50 NM_014670 and W2 domains 1 Nbla10236

NUP54 NM_017426 MGC13407 nucleoporin 54kDa 1 2.31 2.46 1.93 NM_003831 // NM_ DKFZp779L1370 // RIOK3 RIO kinase 3 (yeast) 1 2.59 3.57 2.89 145906 SUDD 55

30 EP 2 136 209 A1

(continued) E7107 (nM) Gene Symbol Accession Synonym Gene Name 0 3 10 30 5 cyclin-dependent CDKN4 // KIP1 // CDKN1B NM_004064 kinase inhibitor 1B 1 1.27 2.35 4.9 P27KIP1 (p27, Kip1)

serine/threonine STK17B NM_004226 DRAK2 1 1.94 3.44 3.99 10 kinase 17b inhibitor of DNA NM_002165 // NM_ binding 1, dominant ID1 ID 1 3.31 6 10.57 181353 negative helix-loop- helix protein 15 GP110 // NM_007002 // NM_ adhesion regulating ADRM1 MGC29536 // 1 1.8 2.68 2.59 175573 molecule 1 Rpn13 eukaryotic DDX2A // EIF-4A // 20 EIF4A1 NM_001416 translation initiation 1 2.17 3.64 4.36 EIF4A factor 4A, isoform 1

XM_001134363 // FOXK2 XM_001134364 // ILF // ILF-1 // ILF1 forkhead box K2 1 2.1 2.68 2.31 25 NM_004514 guanine nucleotide Gnb2-rs1 // H12.3 // binding protein (G GNB2L1 NM_006098 HLC-7 // PIG21 // 1 2.47 2.74 2.23 protein), beta RACK1 polypeptide 2-like 1 30 CSA // GRP75 // HSPA9B // heat shock 70kDa HSPA9 NM_004134 MGC4500 // MOT // 1 1.87 3.45 2.33 protein 9 (mortalin) MOT2 // MTHSP75 // PBP74 // most-2 35 DKFZp686M05240 // HSP105 // HSP105A // heat shock 105kDa/ HSPH1 NM_006644 1 1.26 1.88 2.68 HSP105B // 110kDa protein 1 40 KIAA0201 // NY- CO-25 FLJ13703 // kelch-like 18 KLHL18 NM_025010 1 2.36 2.97 2.6 KIAA0795 (Drosophila)

45 CVIL // CVL // DKFZp782H157 // VIL2 NM_003379 villin 2 (ezrin) 1 1.27 2.87 4.89 FLJ26216 // MGC1584

50 Example 5: Analysis in PBC

[0153] Since fractionation of hemocytes is required for emptying PBMC, use of PBMC in a clinical test is complicated. If change of pre-mRNA can be confirmed in whole blood (PBC), such a test would be clinically more useful. However, since it is difficult to culture PBC, it is not easy to monitor the change of pre-mRNA in vitro. If expression of mRNA in 55 PBC, like in PBMC, is confirmed, the change of pre-mRNA can be monitored. Accordingly, in regard to the genes of Table 2 confirmed for PBMC (DNAJB1, BZW1, NUP54, RIOK3, CDKN1B, STK17B, and ID1), it is examined whether mRNA can be detected for RNA obtained from PBC by the same RNA purification method as in the clinical setting

31 EP 2 136 209 A1

(Tempus PAX gene).

(1) Preparation of RNA with Tempus Blood RNA Tube (Applied Biosystems)

5 [0154] Human peripheral blood was collected in the tube (3ml/tube) and combined with Stabilizing Reagent. In accordance with the protocol of the Tube, RNA was purified by the RNA Blood-DNA Method in ABI 6100 PrepStation (Applied Biosystems). Absorbance at 260nm was measured to quantify an amount of RNA.

(2) Preparation of RNA with PAXgene Blood RNA Tube (QIAGEN) 10 [0155] Human peripheral blood was collected in the tube (2.5ml/tube), combined with Stabilizing Reagent, and left to stand overnight at room temperature. In accordance with the protocol of the Tube, RNA was purified with PAXgene Blood RNA Kit (QIAGEN). Absorbance at 260nm was measured to quantify an amount of RNA.

15 (3) Quantification of the expression level of mRNA

[0156] RNA was prepared to 30 ng/PL and cDNA was synthesized by using High Capacity cDNA Reverse Transcription Kits (Applied Biosystems). A probe corresponding respectively to DNAJB1, BZW1, NUP54, RIOK3, CDKN1B, STK17B, ID1 and 18S rRNA was purchased from TaqMan Gene Expression Assays (Applied Biosystems). Reagents were pre- 20 pared in accordance with the protocol of TaqMan Universal PCR Master Mix (Applied Biosystems) and the expression level of mRNA was measured with ABI7900 (Applied Biosystems). As shown in Figure 3A (Tempus Blood RNA Tube) and Figure 3B (PAXgene Blood RNA Tube), it was demonstrated that gene expression could sufficiently be confirmed in RNA obtained by both methods.

25 Example 6: Analysis by Western blotting

[0157] Since pre-mRNA contains a part of the introns, a protein translated from such pre-mRNA is one which does not normally exist. Consequently the protein may serves as a protein marker to monitor the action of (8E,12E,14E)-7-((4- cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16, 20-pentamethyl-18,19-epoxytric osa- 30 8,12,14-trien-11-olide. Whether the pre-mRNA-dependent abnormal protein practically emerged upon the treatment of (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19- epoxytric osa-8,12,14-trien-11-olide was examined by using cancer cells (HaLa). As a result, insertion of a intron sequence was found to introduce a termination codon, which led to generation of small-molecule p27 and SMN different from normal CDKN1B (p27) (Figure 4). Based on these findings, the protein generated from pre-mRNA can serve as the 35 marker as well. [0158] About 3x105cells of HeLa cells were first seeded in a 24-well culture plate (bottom area: 2 cm2), and 18 hours later, the compound was added thereto at the indicated concentration, followed by additional 24-hour culturing. The cells were washed once with PBS(-), and then were lysed by treating with 0.2mlof M-PER reagent (PIERCE) for 30 minutes. The collected lysate was filtered with a 0.45Pm filter to remove insoluble matters and then combined with an equal 40 amount of 2xSDS-PAGE sample solution. The mixture was heated to be denatured at 95 °C for five minutes to yield a sample to be analyzed. [0159] The analysis sample (15Pl each) was separated with 5-20% SDS-PAGE and transferred onto a PVDF membrane (Hybond-P: GE-Amersham). The membrane was treated to be blocked with Blockace (Dainippon Pharma Co., Ltd.) by one-hour incubation. The membrane was then incubated with a primary antibody for two hours, washed three 45 times for 10 minutes each, incubated with a secondary antibody for one hour, washed (10 minutes each) three times followed by signal detection. [0160] Detection of p27/Kip1 was carried out as follows. Specifically, a mouse anti-p27/Kip1 monoclonal antibody (BD Bioscience, #610242) was used as the primary antibody at a 1:1000 dilution rate. An HRP-labeled mouse anti-IgG antibody (GE-Amersham) was used as the secondary antibody at a 1:2500 dilution rate. An ECL-Plus reagent (GE- 50 Amersham) was used for the signal detection. [0161] Detection of SMN was carried out as follows. Specifically, a mouse anti-SMN monoclonal- antibody (BD Bio- science, #610646) was used as the primary antibody at a 1:1000 dilution rate. An AP-labeled mouse anti-IgG antibody (CHEMICON) was used as the secondary antibody at a 1:2500 dilution rate. NBT/BCIP reagent (PIERCE) was used for signal detection. 55 [0162] As shown in Figure 4, only a 27 kDa band was detected for p27/Kip1 when the cells were treated without the compounds. On the other hand, appearance of a band with about 22 kDa was confirmed in the cells treated with about 100nM of Pladienolide B or (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy- 6,10,12,16,20-pentamethyl-18,19-epoxytric osa-8,12,14-trien-11-olide for 24 hours. In addition, only a 35 kDa band was

32 EP 2 136 209 A1

detected for SMN in the cells treated without the compounds. When the cells were treated with 10nM and 25nM of Pladienolide B or 10nM and 100nM of (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16, 20- pentamethyl-18,19-epoxytric osa-8,12,14-trien-11-olide for 24 hours, multiple bands with a molecular weight of less than 35 kDa were confirmed. 5 Example 7: Analysis in a nude mouse

(1) Administration of the pladienolide derivative to nude mice subcutaneously transplanted with WiDr human colon carcinoma cells. 10 [0163] Nude mice (BALB/cAJcl-nu/nu, 6 weeks old, female) were purchased from CLEA Japan, Inc. After an acclimated period of a week, the mice were subcutaneously transplanted WiDr cells suspended in Hanks’ Balanced Salt Solution (GIBCO) (5x106 cells per a mouse). Two weeks after the transplantation, when tumor volume was confirmed to grow to more than 200 mm3, the mice were administrated (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21- 15 tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytric osa-8,12,14-trien-11-olide (30 mg/kg) in a single dose via tail vein injection.

(2) Blood collection and isolation of the tumor

20 [0164] At the time point of 30 minutes, 1 hour, 2 hours, 4 hours, and 8 hours, after the administration of (8E,12E,14E)- 7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytric osa- 8,12,14-trien-11-olide, two mice per each time point were put down by euthanasia with CO2. Whole blood (with heparin added) was taken from abdominal aorta of each mouse, TRIzol LS Reagent (Invitrogen) was added thereto, and the mixture was stored at -20°C. The tumor was removed, cut in shape of a about 0.5 cm x 0.5 cm square, and stored -20°C 25 in RNAlater (Ambion).

(3) Preparation of RNA

[0165] RNA preparation from blood was carried out in accordance with the protocol of TRIzol LS Reagent (Invitrogen). 30 The obtained RNA was further purified with RNeasy (QIAGEN). During the process, a treatment with DNase I was performed in accordance with the protocol. The tumor treated with RNA later (Ambion) was placed in TRI reagent (SIGMA) and grinded by a homogenizer, followed by the operations following the protocol of TRI reagent. The obtained RNA was then purified using RNeasy (QIAGEN). During the process, a treatment with DNase I was performed in accordance with the protocol. Absorbance at 260nm was measured to quantify an amount of each RNA. 35 (4) Measurement of the expression level of the precursor gene (pre-mRNA) in blood

[0166] RNA was prepared to 100ng/Pl and cDNA was synthesized by using TaqMan Reverse Transcription Reagents (Applied Biosystems). For the expression level of pre-mRNA of mouse DNAJB1 and mouse EIF4A, reagents were 40 prepared in accordance with each protocol by using POWER SYBR GREEN PCR MASTER MIX (Applied Biosystems) and primers with the sequence below (Invitrogen), and the expression level was measured with ABI7900 (Applied Biosystems). The expression level of 18S rRNA was measured by using 18S primers included in TaqMan Ribosomal RNA control reagents (4308329: Applied Biosystems). Measured values were corrected using the expression level of 18S rRNA as an internal control. The expression level of each gene was calculated with the expression level in the group 45 of mice treated without (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy- 6,10,12,16,20-pentamethyl-18,19-epoxytric osa-8,12,14-trien-11-olide as 1. Results were shown in Figure 5.

[mouse DNAJB1]

50 [0167]

Sense: 5’-TGCTGTGAGAATAATGGGTTGTG-3’ (SEQ ID NO: 46) Antisense: 5’-GGCTGGCTTAGGAGCTTCACT-3’ (SEQ ID NO: 47)

55 [mouse EIF4A1]

[0168]

33 EP 2 136 209 A1

Sense: 5’-ACCTGCGGTTCCCACTTTATT-3’ (SEQ ID NO: 48) Antisense: 5’-ACCACTCCAAATGTCTAAGGTCACT-3’ (SEQ ID NO:49)

(5) Measurement of the expression level of the precursor gene (pre-mRNA) in tumor 5 [0169] RNA was prepared to 100ng/Pl and cDNA was synthesized by using TaqMan Reverse Transcription Reagents (Applied Biosystems). For the expression level of pre-mRNA of human DNAJB1 and human EIF4A, reagents were prepared in accordance with each protocol by using POWER SYBR GREEN PCR MASTER MIX (Applied Biosystems) and primers with the sequence below (Invitrogen), and the expression level was measured with ABI7900 (Applied 10 Biosystems). The expression level of 18S rRNA was measured by using 18S primers included in TaqMan Ribosomal RNA control reagents (4308329: Applied Biosystems). Measured values were corrected using the expression level of 18S rRNA as an internal control. The expression level of each gene was calculated with the expression level in the group of mice treated without (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy- 6,10,12,16,20-pentamethyl-18,19-epoxytric osa-8,12,14-trien-11-olide as 1. Results were shown in Figure 6. 15 [Human DNAJB1]

[0170]

20 Sense: 5’-GGCCTGATGGGTCTTATCTATGG-3’ (SEQ ID NO: 50) Antisense: 5’-TTAGATGGAAGCTGGCTCAAGAG-3’ (SEQ ID NO: 51)

[Human EIF4A1]

25 [0171]

Sense: 5’-GAACTTTGCCTCATTCTTTTGCA-3’ (SEQ ID NO: 52) Antisense: 5’-CTGAGCTCCAGTCTCTTGTATTTCTG-3’ (SEQ ID NO: .53)

30 Example 8: Analysis with microarray (2)

[0172] Analysis conditions were reviewed in the data used in Example 3. Genes containing increased introns upon treatment with (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytric osa-8,12,14-trien-11-olide were identified. 35 [0173] In order to consider the analysis conditions, variations in the data from the samples with identical conditions were studied. Figure 7 shows a scatter diagram of the expression level of probe sets and genes of the control cells, and standard deviation thereof. It turned out that, by analyzing under conditions where the expression level was more than 100 and change in the expression level was more than five times, a probe set with increased expression can be extracted. [0174] Probe sets showing that the normalized change in the level expression of the probe set in the group with the 40 treatment was more than 5 times; the expression level of the probe set and the gene in the group with the treatment were more than 100; and probe set annotation was "extended, full, free", were picked out. Welch’s t-test was conducted with the probe sets extracted for the treated group and the control group to determine a p and q value. A gene containing the probe sets with the q value of less than 5% was determined as a candidate gene with increased expression level of the intron regions (Table 3). 45 [0175] In Table 3, for each gene evaluated, gene name (Gene Name), abbreviated name (Gene Symbol), accession number (Accession), alias name (Synonym), transcription cluster number in Human Exon 1.0 ST Array (Human Exon 1.0 ST Array Transcript Cluster ID), chromosome number (Chromosome), type of strand (Strand), start region (Start), stop region (Stop), and change in expression level (Fold Change) were respectively shown.

34 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3139035 chr8 - 68250009 68418446 21.19 3284188 chr10 - 33211051 33321367 21.20 3289031 chr102556302 chr2 -3607698 chr15 51180787 - 512933823519119 + 28.32 64173290 chr13 64225291 87857353 27.36 87975281 - 26.27 78783968 78878613 21.52

30 [Table 3] [Table

35 ARFGEP1 // BIG1 // BIG1 // ARFGEP1 // D730028018Rik // DKFZP434L057 P200 CD29 // FNRB // // CD29 // MDF2 // GPGA // VLAB MSK12 MGC22767 // // MGC22767 // // TIM23 PR01197 TIMM23B DKFZp686C18116 MGC50990 // // FLJ41618 MGC45866 // C13orf10 // FLJ20957 // MGC133295 // MGC133296 // PRO1777 RP11-255E21.1 // SE70-2

40 002211 002211 033667 006421 006327 020651 152258 02211 033669 033669 NM_ // NM_ // 033666 NM_ // NM_ // 033668 NM- 133376 NM // XM_ // 001133798 NM_

45 ARFGEF1 NM_ PELI1C15orf42 NM_ NM_ RBM26 NM_ ITGB1 TSR1TIMM23 018128 NM // FLJ10534 3740998 chr17 - 2172438 2187551 44.77

50 (brefeldin (brefeldin

55 Gene NameGene Symbol Gene Accession Synonym ribosylation factor factor ribosylation inhibited) exchange factor 1 factor exchange A- ADP- nucleotide- guanine pellino homolog 1 (Drosophila) chromosome 15 open 42 frame reading RNA binding motif protein 26 integrin, beta 1 (fibronectin polypeptide, beta receptor, includes CD29 antigen MSK12) MDF2, TSR1 rRNA , 20S accumulation, inner of translocase mitochondrial membrane (yeast) homolog 23

35 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3614087 chr15 - 23006655 23355108 19.35 3819880 chr192515627 + chr2 9112073 + 9135082 19.64 173000563 173079416 19.59 3581386 chr143636956 chr15 - - 104546975 104585458 20.39 82987018 82998719 20.03 2883609 chr53591909 - chr15 157145339 + 157284818 20.51 42506834 42607712 20.40

30 (continued)

35 6 ANCR // AS // E6- AS // ANCR // // // EPVE6AP AP // FLJ26981 HPVE6A CD49f // ITGA6B // // ITGA6B // CD49f VLA- KIAA1588 // // KIAA1588 // DKFZp572C163 // FLJ32813 MGC35232 FLJ20764 // HEPP // FLJ20764 MGC19517 // // FLJ14888 HSPC264 COUNT // ENTH // // COUNT // EPNR EPN4 // EPSINR KIAA01 71 // FLJ10523 // HSPC058 HSPC129 001 001 40 000210 000210 000462 30839 020933 020933 033160 017955 017955 032856 014666 016396 NM_ // NM_ 079818 NM_ // NM_ // 130838 NM_ NM_ XM_ // // 001125688 NM_ NM_ // NM_ 145701

45 UBE3A ZNF317 // // ZNF317 ZNF658 CTDSPL2 NM_ CDCA4

50 terminal

55 Gene NameGene Symbol Gene Accession Synonym integrin, alpha 6 alpha integrin, E3A ligase protein ubiquitin E6- virus papilloma (human protein, associated ITGA6 Angelman syndrome) WD repeat domain 73 domain repeat WD WDR73 // zinc 317 protein finger zinc 658 protein finger NM_ clathrin interactor 1 interactor clathrin CTD (carboxy- CLINT1 polymerase RNA domain, II. polypeptide A) small 2 like phosphatase NM_ cell division cycle associated 4

36 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3662387 chr162510485 + chr22468811 55523269 + 55552122 chr2 19.03 1519746742333136 + 152072768 chr1 18.85 3238491 9264345 chr10 + 9463243 18.43 43597180 + 43601431 22650103 18.22 22660820 18.11 3497586 chr132963784 + chr6 96672563 96844371 - 19.31 88441297 88476721 19.23

30 (continued) alpha alpha

35 HERP // KIAA0025 KIAA0025 HERP // // SUP Mif1 // // DKFZp781N1478 FLJ12870 // AMAP2 // FLJ42910 PAG3 // KIAA0400 Pap- PAP // // SHAG1 // // CDC20A // MGC102824 // bA276H19.3 p55CDC // MGC12685 PCGF4 // RNF51 DKFZp781H1296 // DKFZp781H1296 // // MBLL39 MBLL // MGC120625 // MGC120626 // MGC120628 PR02032 // FLJ10342 dJ486L4.2

40 014685 018151 003887 001255 005180 144778 144778 018064 NM_ // 001010989 NM_ // 001010990 NM_ NM_ // NM_ 207304

45 RIF1DDEF2 NM_ NM_ CDC20 NM_ BMI1 NM_ C6orf166 NM_ HERPUD1 MBNL2 50 inducible, like 2 2 like

55 Gene NameGene Symbol Gene Accession Synonym inducible, ubiquitin- inducible, RAP1 interacting factor factor RAP1 interacting (yeast) homolog development and enhancing differentiation 2 factor 20 cycle division cell (S. cerevisiae) homolog finger ring polycomb BMI1 oncogene chromosome 6 open open 6 chromosome 166 frame reading homocysteine- reticulum endoplasmic stress- 1 member domain like (Drosophila) museleblind-

37 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3890555 chr20 +2694644 chr3 553594932529546 55386992 chr2 - 16.46 + 130369369 130385467 16.43 223433916 223539136 16.27 3261544 chr103476130 + chr12 103993260 104132642 - 17.47 122342423 122435284 17.44

30 (continued)

35 FLJ30608 // // FLJ30608 // MGC117333 // MGC126076 // MGC126077 // // MRNP41 MIG14 // dJ481 Mnrp41 dJ800J21.1 // F12.3 // // DM2 CNBP1 RNF163 PROMM // ZNF9 // ZCCHC22 // // // FACL3 ACS3 PRO2194 FLJ21263 // // FLJ21263 // FLJ21500 // KIAA0248 // MGC134877 MGC134878 // FLJ10701 // FLJ10833 MOP3 // FLJ16176 Sno //

40 004457 004457 003610 003418 004193 018183 174907 MGC131930 018321 1100FLJI BRIX 003902 2629693 // FUBP FBP 2806231 chr3 chr5 2419235 + chr1 + 73019946 - 34951248 73201035 34962845 17.19 78182330 17.08 78217881 16.59 NM_ 203372 NM // NM_ // 001015885 NM_

45 CNBP NM_ ACSL3 GBF1 NM_ SBNO1 NM_ PPP4R2 NM_ FUBP1 NM_ RAE1 50

55 Gene NameGene Symbol Gene Accession Synonym type zinc finger, finger, zinc type specific brefeldin A brefeldin specific CoA synthetase long- CCHC- protein binding acid nucleic acyl- chain family member 3 member family chain golgi- 1 factor resistance homolog notch strawberry (Drosophila) 4, phosphatase protein 2 subunit regulatory 2 containing domain brix element upstream far BXDC2 1 protein (FUSE) binding NM_ 1 export RNA RAE1 (S. pombe) homolog

38 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2476219 chr2 +3453319 32435095 chr12 326974473960629 15.96 - chr22 47509816 - 475323223337618 15.78 37202800 chr11 37232288 15.42 + 67984785 68173381 15.25 3194338 chr9 + 138424942 138438030 16.01

30 (continued) MPP // MPP 2 // NIP2 2 // 3627076 chr15 - 57742025 57768916 15.96 35 APOLLON // BRUCE // // FLJ13726 // FLJ13786 KIAA1289 // MGC8416 // PRPF28 U5-100K prp28 // // DKFZp761H2016 RH70 // P72 // C11orf23 DKFZp781E17107 DKFZp781E2374 // DKFZp78102362 // // FLJl1058 // // FLJ43065 // MGC125711 // MGC125712 // SAP190 // PP6R3 // SAPLa SAPL Alpha- // INPP5E // KIAA0123 MGC104197

40 006386 006386 016252 004330 BNIP- 004818 018312 015160 NM_ // NM_ 030881

45 09 015939 NM MGC5029 3896524 chr20 - 5865881 5879370 16.01 BNIP2 NM_ SAPS3 NM_ BIRC6 NM_ DDX23 NM_ DDX17 PMPCA NM_

50 Asp) Asp) Asp) Ala- Ala- Glu- Glu-

55 Gene NameGene Symbol Gene Accession Synonym 09 protein 09 CGI- baculoviral IAP repeat- IAP baculoviral E1B BCL2/adenovirus 19kDa interacting protein 2 DEAD (Asp- DEAD (Asp- family, SAPS domain member 3 containing 6 (apollon) containing 23 polypeptide box 17 polypeptide box peptidase (mitochondrial (mitochondrial peptidase processing) alpha CGI-

39 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3403045 chr123835645 + chr19 6903897 + 6921744 49839030 14.70 49860075 14.67 2621275 chr3 +3333226 chr11 47298888 47367590 + 15.00 613129293572041 61350560 chr14 14.75 - 74189599 74249655 14.49 2556752 chr2 - 65391279 65513247 15.03 2894663 chr6 + 10799016 10817955 15.04

30 5 // 5 // (continued) 2

35 // MF1 1 // B37 // D12S755E // // D12S755E // B37 // NOD DRPLA HVED // // CD155 Necl- // NECL5 PVS // TAGE4 FLJ13703 // // FLJ13703 KIAA0795 FEN- RAD2 FLJ20624 // MAK11 MAK11 // FLJ20624 // RP11- PIP1 // // WDR84 421M1.5 // bA421M1.5 // hPIP1 // FLJ22324 // MGC90272 // // bA526K24.2 dJ842G6.1 // FLJ21897 // FLJ31917 // MGC163164 Spred-

40 006505 025010 003171 SUV3 014761 MGC117220 004111 3667766 3250204 chr16 chr10 + + 70481983 70609946 70522196 70638996 14.78 14.99 017906 017906 024120 181784 NM_ // 001007026 001940 NM NM_ 001039479 NM_ // NM_ // 001039375 NM_

45 SUPV3L1 NM_ FEN1 NM_ SPRED2 NM_ PAKlIP1 // PAKlIP1 C20orf7 50 like 1 like

55 related, EVH1 related, Gene NameGene Symbol Gene Accession Synonym like 18 (Drasophila) KLHL18 NM_ poliovirus receptorpoliovirus KIAA0317 PVR NM_ K1AA0317 suppressor of var1, 3- var1, of suppressor (S. cerevisiae)structure- flap KLAA0174 endonuclease specific 1atrophin 1 K1AA0174 NM_ ATN1 kelch- sprouty- 2 containing domain PAK1 interacting protein 1 // 1 // protein interacting PAK1 chromosome 20 open 7 frame reading

40 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3956854 chr22 - 28224935 28280423 14.15 2367287 chr1 + 170017287 170053841 14.17 3974838 chrX2921374 chr6 +3352503 41055591 + chr11 41108668 111409800 14.39 + 111458743 14.38 119711882 119896306 14.21

30 (continued) 1 // ILF1 1 3738969 chr17 + 78070883 78195807 14.01

35 01 // FLJ10310 C22orf19 // Fmip // Fmip // C22orf19 PK1.3 //ILF- ILF 5630401 D24Rik // D24Rik 5630401 CGI- DBX // DDX14 // DDX14 DBX // // HLP2 DDX3 // RPF2 FLJ21087 bA397G5.4 // DKFZp68602372 LARG // KIAA0382 PRO2792 // 40 003678 006622 SNK 2858023 chr5 - 57785572 57792624 14.01 015935 001356 032194 001102 FLJ40884 015313 3569814 chr14 - 68409817 68515815 14.26 XM_ // 001134363 XM_ // 001134364 004514 NM NM_ // 001002877 NM_ // 001002878 NM_ // 001002879 NM_ NM_ 001007239 11 NM_ // 014955 NM_ XM_ // 001129278 NM_

45 PLK2 NM_ ARHGEF12 NM_ DDX3X

50 linked Asp) Asp) Ala- Glu-

55 Gene NameGene Symbol Gene Accession Synonym like kinase 2 polo- (Drosophila) K2 box forkhead FOXK2 THO complex 5 THOC5 brix domain containing 1 containing domain brix BXDC1 1 alpha actinin, nucleotide guanine Rho 12 (GEF) factor exchange NM_ ACTN1KlAA0859 NM_ K1AA0869 DEAD (Asp- box polypeptide 3, X- polypeptide box

41 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2812435 chr5 + 652580793886639 65451372 chr20 13.87 + 42927275 42970748 13.72 3781654 chr18 + 19161035 19320545 13.87 2531522 chr22745499 chr4 +3766960 chr17 + 231285781 231394027 13.97 - 144325529 144364549 13.94 59968891 60088896 13.92

30 (continued) 1

35 // FLJ22682 66 ERBIN // LAP2 // // LAP2 ERBIN MCH2 // HSt GW128 KCIP- DKFZp779L1370 // // DKFZp779L1370 SUDD CGI- MO25 // // FLJ35970 // HP43.8KD KIAA1691 // DKFZp686F0270 MGC138150 40 003404 003404 003831 003831 018695 032992 032390Nopp34 // NiFK 2573786 chr2 - 122132489 122231052 13.76 002710 PPP1G 3471374 chr12 - 109642007 109665131 13.87 016289 032557 022739 NM_ // NM_ 139323 NM_ // NM_ 145906 NM_ // 001006600 NM_ // NM_ // 001226 NM_

45 MKI671P NM_ YWHAB PPP1CC NM_ ERBB21P // ERBB21P CASP6 USP38SMURF2 NM_ NM_

50 55 Gene NameGene Symbol Gene Accession Synonym MKI67 (FHA domain) nucleolar interacting phosphoprotein 3- tyrosine monooxygenase/ tryptophan 5- tryptophan activation monooxygenase protein, protein phosphatase 1, phosphatase protein gamma subunit, catalytic isoform // protein interacting erbb2 apoptosis- 6, caspase related cysteine peptidase cysteine related calcium binding protein 39 protein binding calcium CAB39 peptidase specific ubiquitin 38 NM_ E3 ubiquitin specific SMAD 2 ligase protein 3 (yeast) kinase RIO RIOK3

42 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2548776 chr22542816 - chr2 38374621 - 38516141 13.57 20291440 20450197 13.55 3606304 chr15 +2394784 chr1 83681343 84102785 - 13.65 6504004 6537329 13.58 3320301 chr11 +3724782 chr17 10684027 10774985 + 13.68 43082272 43117868 13.68

30 3 // 3 (continued) LB // c- // LBC Lbc // BRX // BRX // // Lbc 35 ARL3IP2 // ATL2 // // // ATL2 ARL3IP2 // FLJ23293 atlastin2 // FLJ36528 // KLAA0235 // MGC138251 // MGC138253 PUML2 // PUMH2 AKAP- // FLJ11952 // HA- FLJ43341 LBC // // Ht31 PROTO- PROTO- Ibc // FLJ23323 // MGC131821 MGC138483 KIAA0155 // // KIAA0155 TSBP // // SH2BP1 // // p150TSP p150 // MGC99627 // MTU1 // MTO2 // TRMT1 // TRMT TRNT1 // // IPOB IMB1 // MGC2155 lmpnb // MGC2156 // NTF97 // MGC2157 40 022374 015317 006738 006738 144767 024654 014633 014633 002265 NM_ // NM_ // 007200 NM_ NM_ // NM_ 018006

45 PUM2 NM_ ARL61P2 NM_ KPNB1 NM_ AKAP13 CTR9 // CTR9 // TRMU

50 like 2-

55 Gene NameGene Symbol Gene Accession Synonym ribosylation factor- ribosylation pumilio homolog 2 homolog pumilio (Drosophila) 6 interacting protein 2 protein 6 interacting nucleolar protein 9 protein nucleolar ADP- NOL9 NM_ karyopherin (importin) beta beta (importin) karyopherin 1 (PRKA) anchor A kinase 13 protein methylaminomethyl- Ctr9, Paf1 /RNA Paf1 Ctr9, complex II polymerase (S. homolog component, cerevisiae) // tRNA 5- thiouridylate methyltransferase

43 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3385175 chr11 - 85345353 85458481 13.00 2929036 chr6 +3755714 chr17 144194149 144227146 13.35 - 34801544 34861069 13.29 2551924 chr2 - 47232159 47286178 13.54

30 (continued)

35 CALM // CLTH // CLTH // CALM LAP - 2421271 chr1 - 87100720 87153273 13.02 dJ468K18.5 // dJ468K18.5 // C6orf93 // FLJ14909 dJ488K18.4 CRSP200 // CRSP1 // DRIP205 // // // MEND DRIP230 // PBP MGC71488 PPARGBP // // TRAP220 RB18A TRIP2 // GAR1 2739242 chr4 + 110956115 110965340 13.42 CAMII // PHKD // // CAMII PHKD2 40 007166 002809 S3 // RPN3 // P58 3720636 chr17 + 35390438 35407732 12.85 004261 004261 032860 004774 000859 - 2815965 chr5 + 74668800 74700136 13.12 018983 018983 001743 928657 928657 NM_ // 001008660 NM_ NM_ // NM_ 203341 XM_ XM_ // // 941265 NM_ NM_ // NM_ 032993

45 Sep PSMD3 NM_ PICALM HMGCR NM_ C6orf94 // LTV // LTV C6orf94 1 CALM2 NM_ NOLA1

50 Coenzyme 3- 55 Gene NameGene Symbol Gene Accession Synonym ATPase, 3 ATPase, hydroxy- proteasome (prosome, (prosome, proteasome subunit, 26S macropain) non- phosphatidylinositol phosphatidylinositol assembly clathrin binding protein PPAR binding proteinPPAR binding PPARBP3- methylglutaryl- NM_ A reductase selenoprotein kDa 15 15- chromosome 6 open open 6 chromosome LAV1 // 94 frame reading (S. cerevisiae) homolog calmodulin 2 2 calmodulin kinase, (phosphorylase delta) A, family protein nucleolar 1 small (H/ACA member RNPs) nucleolar

44 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3623424 chr152420808 - chr12981912 47203877 - chr6 47235198 12.73 85504067 - 855161713250055 12.67 chr10 159106770 1591604323319937 12.62 + chr11 703805843326252 + 70414821 chr11 12.56 9550916 + 9579143 12.54 34083688 34125769 12.51

30 (continued) E10 // // E10

35 // RH- II/GU ALIEN // CSN2 // CSN2 // ALIEN // TRIP15 SGN2 CARMEN // CIPER c- CLAP // // mE10 // // CVL CVIL // DKFZp762H157 // FLJ26216 MGC1584 DKFZp686F21172 // GUA // GURDB // RH- II/GuA // DKFZp686I18166 // FLJ16446 WEE1hu // ALP // DKFZp434C116 // FLJ10774 // FLJ12179 // FLJ23850 hALP // KIAA1709

40 004236 003921 003379 004728 003390 024662 003198TCEB3A // SIII 2325251 chr1 + 23942459 23961135 12.38

45 COPS2 NM_ SLC25A32 030780 NM DDX21 MFTC // FLJ23872 3147726 chr8 NM_ - 104247068 104496640 12.60 TCEB3 NM_

50 Asp) Asp) Als- Glu- lymphoma 10 lymphoma BCL10 NM_ 55 Gene NameGene Symbol Gene Accession Synonym acetyltransferase 10 acetyltransferase NAT10 NM_ cell CLL/ COP9 constitutive constitutive COP9 photomorphogenic 2 subunit homolog (Arabidopsis) B- 2 (ezrin) villin 25, family carrier solute 32 member VIL2DEAD (Asp- 21 polypeptide box NM_ pombe) (S. homolog WEE1 WEE1 NM_ N- elongation transcription 3 B (SIII), polypeptide factor elongin (110kDa,

45 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3233322 chr10 + 5766851 5846629 12.16 3151473 chr8 - 124291083 124356860 12.17 2407191 chr1 - 37805043 37834120 12.14 3882069 chr203781531 chr18 +3320604 chr11 + 308713043228191 30901864 + 18940699 chr9 12.37 19101596 11819556 12.37 - 11937446 12.32 134456969 134535609 12.21

30 (continued) 1 // 1 //

35 DKFZp781E1986 // DKFZp781E1986 // FLJ20360 bA318E3.2 FLJ14825 // // FLJ14825 - // MGC9784 FLJ40906 // // FLJ40906 // HUMAUANTIG // Ngp- NGP1 dJ423B22.6 EB1 // MGC117374 // MGC117374 EB1 MGC129946 // // FLJ35924 HsT2563 DKFZp686C13257 // TRFP FLJ20727 // // FLJ13633 // FLJ14578 // FLJ23349 helicain A // helicain C helicain B // 40 032847 032847 007222 022779 022779 012325 38375 017944 374765 374765 013285 XM_ XM_ // 937970 NM_ // NM_ // 001017926 NM_ NM_ // NM_ 138620

45 C10orf18 GNL2 NM. MAPRE1 NM_ CABLES1 NM_ USP47 NM_ // C8orf78 ZHX1 DDX31

50 Asp) Asp) Ala- associated Glu-

55 like 2 (nucleolar) 2 like Gene NameGene Symbol Gene Accession Synonym guanine nucleotide binding binding nucleotide guanine protein- chromosome 10 open 18 frame reading microtubule- family, RP/EB protein, member 1 enzyme Abl and Cdk5 1 substrate peptidase specific ubiquitin 47 DEAD (Asp- open 8 chromosome zinc // 76 frame reading 1 homeoboxes and fingers box polypeptide 31 polypeptide box

46 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3603532 chr15 + 76889894 76979806 11.90 3587457 chr153932270 + chr21 30693622 - 30719422 12.06 39636124 39643423 11.92 3820342 chr19 + 10077989 10082841 12.07 2655688 chr3 + 185514970 185535829 12.13

30 (continued)

35 CSR // CSRB SEN // Eaf3 SEN1 // // // FWP006 // HsT17725 // MGC10631 MORFRG15 // S863-6 // MRG15 GAP (1-12) // GAP (1-12) // KIAA0013 MGC70740 // FLJ27265 // FLJ31471 II HMG14 MGC104230 MGC117425 BXDC3 // BXDC3 // MGC14226 // SSF MGC45852 // SSF2 // SSF1 DKFZp686A1451 // DKFZp686A1451 // // EIF4G EIF4F p220 40 019604 - 3302240 chr10 - 99098933 99175486 11.86 006792 006792 206839 014783 014783 020230 020230 004965 004953 004953 198241 198244 NM_ NM_ // NM_ // 006791 NM_ NM_ // NM_ 199357 NM_ // NM_ 001040664 NM_ // NM- // 182917 NM_ // NM_ // 198242 NM_

45 KIAA0690 // KIAA0690 CRTAM HMGN1 NM_ // MORF4 MORF4L1 ARHGAP11A PPAN // PPAN- P2RY11 EIF4G1

55 Gene NameGene Symbol Gene Accession Synonym mobility group group mobility cytotoxic and regulatory T T regulatory and cytotoxic molecule cell high- binding nucleosome 1 domain 4 // mortality factor mortality factor 4 like 1 Rho GTPase activating 11A protein P2RY11 peter pan homolog homolog pan peter PPAN- // (Drosophila) eukaryotic translation translation eukaryotic 1 gamma, 4 factor initiation

47 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3475511 chr12 - 121257461 121277963 11.73 2741768 chr4 + 122941935 122957724 11.79 3388914 chr11 - 102342328 102485844 11.81

30 (continued) S // 75 // 75 1 // SHAPY 1 3772775 chr17 - 74499403 74517744 11.68

35 EF2 2 // 3846538 chr19 - 3926677 3936451 11.73 ATP1B // MGC1798 // ATP1B 2366422 chr1 + 167342204 167368946 11.44 DIABLO- // FLJ10537 // SMAC FLJ25049 SMAC3 // PM/Scl- // RRP45 PMSCL1 // p6 p5 // Rrp45p // FLJ32431 // // FLJ32431 MGC2714 40 38929 001677 019887 019887 014691 KIAA0560 3617757 chr15 - 32935042 33160557 11.56 001961 EEF- 005033 012461 TIN2 032299 004508IPPI1 // IPP1 3558012 chr14 3273601 chr10 - - 23776465 23781950 11.82 1075869 1092634 11.81 NM_ // 001001787 NM_ NM_ // NM_ // NM_ 138930 NM_ // 001034194 NM_

45 ATP1B1 EEF2CANT1 NM_ 138793 NM SCAN- D1ABLO TINF2DCUN1D5 NM_ NM_ ID11 NM_

50 diphosphate diphosphate

55 Gene NameGene Symbol Gene Accession Synonym moesin (mouse) homolog aquarius AQR A2 receptor EPH Na+/K+ ATPase, 1 beta transporting, polypeptide NM_ EPHA2 MSN 004431 No 002444 NM ECK 2397948 chr1 3979659 chrX - + 16323428 16355151 64804248 11.54 64878488 11.57 eukaryotic translation translation eukaryotic 2 factor elongation activated calcium 1 nucleotidase diablo homolog homolog diablo (Drosophila) TERF1 (TRF1)-interacting (TRF1)-interacting TERF1 2 factor nuclear cullin defective in DCN1, domain 1, neddylation cerevisiae) 5 (S. containing isopentenyl- 9 component exosome EXOSC9 delta isomerase 1 isomerase delta

48 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3656555 ehr16 +3976341 chrX 306811202676726 30695182 chr3 11.42 +3225398 47326654 chr9 -2717757 47332978 11.27 chr4 53296412 - 533566923319840 11.27 + 127036953 127064590 chr11 11.27 84745823191900 + 8545892 chr9 11.25 9362702 + 9426296 11.19 132990780 133102339 11.18

30 (continued)

35 BRE1B // BRE1B // DKFZp686K191 // KIAA0661 // MGC13051 STARING // RBP95 CLGI // EPA // EPO // // HCI FLJ90373 // TIMP // HSA275986 // Nbla00360 SMIF // SMAD4IP1 // // FLJ26106 SIP // MIF2 GRP78 // FLJ12891 FLJ35725 // FLJ14581 // MGC138673 RANBP7 // CAN CAIN // D9S46E // MGC104525 N214

40 014771 014657 003254 018403 3905073 005347 chr20 152544 - 004162 RAB5 36044840 006391 36095268 11.38 2613386 005085 chr3 + 19963571 20002852 11.19

45 TIMP1DCP1A NM_ NM_ HSPA5C4orf23 NM_ RAB5A NM_ NM_

55 protein, regulated Gene NameGene Symbol Gene Accession Synonym ring finger protein 40 protein finger ring RNF40KIAA0406 metallopeptidase TIMP 1 inhibitor NM_ enzyme decapping DCP1 cerevisiae) A (S. homolog KIAA0406 5 protein 70kDa shock heat NM_ (glucose- 78kDa) open 4 chromosome 23 frame reading RAS member RAB5A, oncogene 7importin 214kDanucleoporin IPO7 NUP214 NM_ NM_

49 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3482219 chr13 + 24773258 24822202 10.97 3400625 chr12 + 1670418 1768071 11.05 3740479 chr17 - 1500681 1534906 11.12 2835006 chr53346453 chr11 + 148705190 + 148714338 11.03 101486379 101609466 11.01

30 (continued)

35 KIAA0410 // // KIAA0410 PRO2463 CYK18 // K18 // CYK18 ACDCR2 // // FLJ21432 3415576 // MGC4640 PAQR2 chr12 + 51596769 51632949 11.07 HPRP8 // PRP8 // // PRP8 HPRP8 // RP13 PRPC8 DKFZp451 C205 // // C205 DKFZp451 // FLJ23713 Mt- // FLJ33918 GrpE#2 // // YAP2 YAP YAP65

40 000224 000224 014089 024551 006445 006662 KIAA0309 3656418 chr16 + 30616551 30663998 11.09 003017 SRp20 031966 CCNB 152407 2905118 006106 chr6 2813414 chr5 004289 NRF3 + + 36669658 36741293 68498462 2993590 11.05 68509822 chr7 11.03 + 26158385 26194013 11.01 NM_ 199187 NM // NM_ // 001008564 NM_ // 001008565 NM_

45 PRPF8SRCAP NM_ NM_ GRPEL2 NM_ YAP1NFE2L3 NM_ NM_ SFRS3 NM_

50 related mRNA 55 Gene NameGene Symbol Gene Accession Synonym rich 3 rich like 2, mitochondrial associated protein 1, serine- adiponectin receptor 2 receptor adiponectin ADIPOR2 arginine/ factor, splicing NM_ PRP8 pre- processing factor 8 cerevisiae) (S. Snf2- homolog CBP activator protein 18keratin KRT18 cyclin B1GrpE- (E. coli) Yes- 65kDa CCNB1(erythroid- factor nuclear 3 2)-like derived NM_ 1 like nucleoporin NUPL1

50 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3414390 chr123258168 + chr10 48765279 + 48780742 10.90 94292951 94405130 10.90 2518428 chr23852783 + chr193338192 182464815 chr11 - 1825167323884450 10.95 + chr20 14485622 14501114 69161881 + 10.94 69178408 10.91 36095232 36189576 10.91

30 (continued) 14 3223872 chr9 - 122980236 123025093 10.96

35 // SK 1 3247172 chr10 + 53744067 53807545 10.89 1 // OS1 // // OS1 1 BAF60A // CRACD1 BAF60A // Rsc6p // // HKSP EG5 TRIP5 // KNSL1 CS- // DKFZp31301039 // DKFZp779G0129 // FLJ45996 KRAP // KIAA1927 SPAG13 // // Hdj1 // HSPF1 Hsp40 // BCL1 D11S287E U21B31 // PRAD1 // CREPT // // DKFZp434P0735 // FLJ44520 dJ1057B20.2

40 003076 003076 016322 // RAB- FBP 004523 012242 DKK- 006751 006145 053056 021215 014264 SAK // STK18 2742985 chr4 + 129021450 129039809 10.88 NM_ // NM_ 139071

45 RAB14 NM_ DKK1 NM_ DNAJB1 NM_ C20orf77 NM_ SMARCD1 PLK4 NM_

55 Gene NameGene Symbol Gene Accession Synonym like kinase 4 RAB14, member RAS member RAB14, oncogene kinesin family member 11 member family kinesin KIF11 1 homolog dickkopf laevis) (Xenopus NM_ sperm specific antigen 2antigen specific sperm SSFA2DnaJ (Hsp40) homolog, 1 B, member subfamily NM_ cyclin D1chromosome 20 open 77 frame reading matrix related, SWI/SNF CCND1 actin associated, of regulator dependent d, subfamily chromatin, NM_ member 1 polo- (Drosophila)

51 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3442024 chr12 - 6536290 6547817 10.79 3194635 chr9 + 138810077 138855460 10.81 3191695 chr9 + 132559000 132572797 10.83 2788195 chr4 - 146274170 146471942 10.88

30 (continued) 11 // RIP5 // 11 3883971 chr20 + 34667571 34674368 10.81 35 MGC117384 // MGC117384 // MGC149287 // MGC149288 NSUN1 NOP120 // p120 // MGC15438 // PARF // PARF MGC15438 // RP11-216L13.7 // // RP11-216L13.9 // bA216L13.7 // FLJ10101 // Parf // FLJ13045 // bA216L13.9 pp8875 PNAS- RRP4 // Rrp4p // // // Rrp4p RRP4 // p7 hRrp4p DKFZp434I0721 // DKFZp434I0721 // // HSHIN1 HIN1 KIAA1046

40 006170 018840 018840 024718 017493 017493 014285 005030 // STPK13 PLK 3653072 chr16 + 23597664 23609180 10.82 133368 KIAA1972 3662612 chr16 + 55777703 55831882 10.87 018509 // FLJ21675 3762355 chr17 - 45813504 45836593 10.85 NM_ // 001033714 NM_ NM_ 199483 NM // NM_ // 001039374 NM_ NM_ // NM_ 199324

45 PLK1C20orf24 NM_ // KIAA1984 C9orf86 RSPRY1LRRC59 NM_ M_

55 Gene NameGene Symbol Gene Accession Synonym like kinase 1 nucleolar protein 1, 120kDa 1, protein nucleolar NOL1 exosome component 2 component exosome polo- EXOSC2(Drosophila) chromosome 20 open NM_ 24 frame reading 9 chromosome // KIAA1984 86 frame reading open ring finger and SPRY SPRY and finger ring 1 containing domain repeat rich leucine 59 containing OTU domain containing 4 containing domain OTU OTUD4

52 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3020192 chr73448428 chr12 + - 115637811 115743800 10.53 26949277 26982501 10.50 2903470 chr6 + 33276220 33280187 10.55 2663244 chr3 - 12600117 12680654 10.61

30 (continued) 1 // c- 1 // 2 // TESTIN 2 //

35 DKFZP586B2022 // DKFZP586B2022 TESS // MGC1146 TESS- // // FLJ10630 FLJ10637 D6S115E // D6S115E H2- // D6S2244E KE4 // HKE4 // KE4 // ZIP7 // RING5 // RNF1 CRAF // Raf- CRAF // Raf // DKFZp68612148 // MAP2B MAP2A // MAP2C DKFZP434F2021 2688882 chr3 - 113926517 114253449 10.73 40 015641 015641 006979 0181 64 0181 002880 002880 002374 031847 015412 032482 // KIAA1814 DOT1 3816264 015343 HSA011916 chr19 3743501 + chr17 2114945 2183576 - 10.70 7087644 7096514 10.70 NM_ // NM_ 152829 NM_ // 001077516 NM_ // NM_ 002931 NM_ // NM_ // 001039538 NM_ // NM_ // 031845 NM_ NM_ // 001025072 NM_ // 001025073 NM_

45 C12orf11 NM_ TES SLC39A7 // // SLC39A7 RING1 RAF1 // MAP2 DOT1LDULLARD NM_ NM_ C3orf17

50 associated

55 Gene NameGene Symbol Gene Accession Synonym like, histone H3 1 murine leukemia raf- chromosome 12 open 11 frame reading testis derived transcript (3 (3 transcript derived testis UM domains) solute carrier family 39 (zinc 7 // member transporter), 1 protein finger ring viral oncogene homolog 1 // 1 homolog oncogene viral microtubule- protein 2 protein DOT1- (S. methyltransferase cerevisiae) (Xenopus homology dullard laevis) v- chromosome 3 open open 3 chromosome 17 frame reading

53 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3819543 chr19 + 8415651 8459993 10.37 3764103 chr17 - 53421412 53439635 10.37 3639031 chr15 -3510858 89310285 chr133734760 89338950 10.49 chr17 -3715703 chr17 + 40027817 40162098 + 70769374 10.41 70774626 24013260 10.41 24053809 10.38 2971378 chr6 - 117988142 118030384 10.49

30 5 (continued) S7 // S // MRP- S // 35 S7 // RPMS7 S7 DKFZp547H118 // // DKFZp547H118 HNRNPM // HNRNPM4 // HTGR1 HNRPM4 // ASF // MGC5228 // // // MGC5228 ASF // SF2p33 // SF2 SRp30a ASE1 // MGC1671 // MGC1671 // ASE1 // PC4 // MGC3669 TIS7 FKHR // // FKH1 FOXO1 MRP- RP- // K1AA0162 // SPT6 MGC87943 // emb- SPT6H // CAL // FIG // // FIG CAL PIST // // GOPC1 MCF3 // dJ94G16.2 ROS // 31203 40 005968 005968 006924 020399 003981 199414 001550 018146 HC90 // FLJ10581 002015 3705539 chr17 015971 170 + 632263 642481 10.45 NM_ // NM_ NM_ // 001078166 NM_ NM_ // 001017408 NM_ // NM_ 002944 NM_ // NM_ // 199413 NM_ // NM_ // 001007245 NM_

45 HNRPM SFRS1 RNMTL1FOXO1A NM_ MRPS7 NM_ SUPT6H NM_ NM_ PRC1 // PRC1 // IFRD1 GOPC // ROS1

55 Gene NameGene Symbol Gene Accession Synonym rich 1 (splicing factor factor (splicing 1 rich coil motif containing containing motif coil ros UR2 sarcoma virus virus UR2 sarcoma ros heterogeneous nuclear nuclear heterogeneous M ribonucleoprotein serine- factor) splicing alternate 2, RNA methyltransferase like like methyltransferase RNA 1 01A box forkhead (rhabdomyosarcoma) ribosomal mitochondrial S7 protein homolog 6 Ty of suppressor cerevisiae) (S. arginine/ factor, splicing protein regulator of regulator protein // interFeron- 1 cytokinesis related developmental developmental related 1 regulator golgi associated PDZ and and PDZ associated golgi coiled- // v- 1 homolog oncogene (avian)

54 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2908052 chr62444451 + chr13470549 43592769 chr12 - 436050712655511 10.29 chr3 - 172035313 172104622 10.28 107563018 + 107697353 10.27 185386580 185395316 10.26 3233182 chr10 + 54445353120008 5491001 chr8 10.35 + 145205527 145207529 10.30

30 L (continued)

35 RPA39 // RPA40 // RPA40 // RPA39 // RPAC1 RPA5 // Clorf155 CENP- RP3- // FLJ31044 // // 383J4.1 dJ383J4.3 HCRNN4 // coronin- 3 // EST201864 FLJ11198 ARHGEF8 // ARHGEF8 NET1A // RRP41 FLJ20591 Rrp4lp // RRP41A // // // Ski6p SK16 // p12A // hRrp41p

40 004875 004875 033319 014325 018358 018975 // RAP1 DRIP5 3669092 chr16 + 74238853 74353272 10.25 005863 001034 // RR2M R2 013242 GTL3 // EVORF 2469252 019037 3693511 chr2 chr16 018428 + HCA66 // C17orf40 - 3752437 10179982 chr17 56683698 10279478 56739201 10.35 - 10.32 27211153 27252839 10.30 NM_ // NM_ 203290 NM_ // 01047160 NM_

45 CORO1C NM_ TERF2IP NM_ ABCF3 NM_ RRM2C16orf80 NM_ NM_ UTP6POLR1C NM_ NET1

55 Gene NameGene Symbol Gene Accession Synonym binding cassette,sub- centromere protein L protein centromere binding actin coronin CENPL 1C protein, ATP- NM_ binding repeat telomeric protein interacting 2, factor family F (GCN20), member member F (GCN20), family 3 ribonucleotide reductase reductase ribonucleotide polypeptide M2 chromosome 16 open frame reading 4 component exosome 80 EXOSC4 (SSU) subunit small UTP6, component, processome NM_ (yeast) homolog (RNA) I polymerase 30kDa C, polypeptide neuroepithelial cell cell neuroepithelial 1 gene transforming

55 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2928461 chr6 + 142622079 142853981 10.05 3376235 chr113750785 - chr17 62356627 - 62365857 10.13 23928719 23950424 10.12 2834093 chr5 + 145754916 145871713 10.18 3360941 chr113543411 - chr14 64534962855501 + 6459171 chr5 10.24 72594776 72658577 - 10.23 43324231 43349337 10.19

30 (continued)

35 APA1 // 1 3543884 chr14 + 73423093 73468718 10.23 DREG // PS1TP2 // // PS1TP2 // DREG VIGR FLJ10439 // // FLJ10439 FLJ21730 // DEEPEST // MAP126 hMAP126 CA150 // // CA150 // MGC133200 POR1 // GST // // // GST POR1 // MGC26949 // OATP6A1 OATPY // MGC105088 // MGC117168 // S164 RNPC7 HMGCS // MGC90332 40 020455 018093 006461 006706 012402 012402 021239 021188 APA- 002130 NM_ // 001032394 NM_ // 001032395 NM_ // NM_ 198569 XM_ // 001125771 NM_ NM_ // 001040006 NM_ NM_ // NM_ 173488

45 GPR126 RBM25 NM_ HMGCS1 NM_ TCERG1 ARFIP2 // ARFIP2 SLC06A1

50 Coenzyme 3- coupled receptor receptor coupled 55 Gene NameGene Symbol Gene Accession Synonym ribosylation factor factor ribosylation hydroxy- sperm associated antigen 5antigen associated sperm SPAG5 NM_ protein- G 126 WD repeat domain 74 domain repeat WD WDR74 RNA binding motif protein 25 410 protein finger zinc 3- methylglutaryl- ZNF410 1 (soluble) A synthase elongation transcription NM_ 1 regulator ADP- interacting protein 2 carrier solute 2) // (arfaptin transporter anion organic 6A1 member family,

56 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3892565 chr20 + 60245389 60304834 9.91 3629475 chr15 -2434438 63196772 chr1 63213308 9.97 - 148799312 148818878 9.93 3192525 chr9 + 134535243 134581784 10.00

30 2 (continued) L // MKP6 L 3719515 chr17 + 32922795 32947707 9.97

35 5A 3553607 chr14 + 102743652 102881108 10.00 FLJ20223 // // FLJ20223 // KIAA0772 // MGC4307 ORP- // MGC8342 ORP2 // EIF- // HES18 // ES18 MGC22015 // // MCL1L EAT // MCL1S // MGC104264 - // FLJ21002 // MGC138450 // // TFIIIC90 TFIII90 // TFIIICdelta TFiiiC2-90 3184940 chr9 + 113412172 113474576 10.05 40 014835 014835 001969 001969 021960 005707 007026 MKP- 020165 RNF73 2662020 chr3 - 8792108 8980146 9.94 012204 NM_ // NM_ 144498 NM_ // NM_ 183004 NM_ // NM_ 182763 NM_ // 001015882 NM_ 001017998

45 DUSP14RAD18 NM_ NM_ OSBPL2 MCL1 GTF3C4 NM_ EIF5 bA16L21.2.1 bA16L21.2.1 // GNG10 50 related)

55 Gene NameGene Symbol Gene Accession Synonym like protein // guanine guanine // protein like programmed celldeath 7 PDCD7 specificity dual 14 phosphatase homolog (S. RAD18 NM_ cerevisiae) leukemia cell myeloid 1 (BCL2- sequence proteinbinding oxysterol 2 like general transcription factor factor transcription general 90kDa 4, polypeptide IIIC, translation eukaryotic 5 factor initiation DnaJ- protein binding nucleotide 10 gamma protein), (G

57 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3326540 chr11 + 34870003 34998695 9.81 3371719 chr11 -3888217 46721250 chr20 46824660 9.90 + 47237780 47294013 9.83 2468622 chr2 + 8513132 8750492 9.91

30 (continued) TOG

35 43 2320048 chr1 + 10995025 11013170 9.82 DLDBP // E3BP // // E3BP DLDBP PDX1 // // OPDX // FLJ12099 // proX // JNK3 FLJ33785 // JNK3A // MGC50974 // PRKM10 // p493F12 FLJ35359 // // FLJ35359 // TOG // KIAA0097 TOGp // ch- // DKFZp667N057 // FLJ12917 // FLJ20596 // FLJ22238 // HSPC259 // MGC1018 // MGC163147 // // RHLP PP3241 - // GIG8 // ID2A // ID2A // // // GIG8 - // MGC26389 ID2H

40 003477 003477 138980 138982 020175 // FLJ13896 DUS3 3847420 chr19 - 5735867 5759311 9.80 014758 021103 MIG12 017895 2491271 chr2 007375 TDP- + 84959319 84988131 9.85 002166 NM_ // NM_ // 002753 NM_ // NM_ // 138981 NM_ NM_ // 001008938 NM_ NM_ // 001039082 NM_

45 DUS3L NM_ PDHX // MAPK10 DDX27 NM_ CKAP5 ID2B // ID2 ID2B //

50 Asp) Asp) helix helix Ala- loop- Glu-

55 protein activated Gene NameGene Symbol Gene Accession Synonym helix protein // inhibitor inhibitor // protein helix dihydrouridine synthase 3- synthase dihydrouridine like (S. cerevisiae) (S. like kinase 10 kinase thymosin, beta 10 beta thymosin, TMSB10DEAD (Asp- NM_ bindingTAR DNA protein TARDBP dehydrogenase pyruvate NM_ X // component complex, mitogen- box polypeptide 27 polypeptide box cytoskeleton associated associated cytoskeleton 5 protein inhibitor of DNA binding 2B, of DNA binding inhibitor helix- negative dominant loop- 2, dominant binding DNA of helix- negative protein

58 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3508330 chr133666686 - chr16 30558258 + 30651692 9.68 67930869 67935044 9.64 3333358 chr11 + 61648046 61677757 9.73 2695200 chr3 -3156193 chr8 131801268 132026111 9.79 - 141599440 141726037 9.74

30 (continued)

35 // FLJ10296 37 MAN1B //-MAN1B 2353881 chr1 + 117689854 117931990 9.61 DKFZp686M05240 DKFZp686M05240 // HSP105 // // HSP105A // HSP105B NY- // KIAA0201 CO- 25 CGI- KD93 // HSPC031 // FLJ31633 // // FLJ31633 MGC111393 MGC102700 // MGC102700 p150 // VPS15 AGO2 // MGC3183 //Q10

40 006699 006699 006644 016101 001432 ER 2731513 chr4 + 75440309 75473341 9.62 005507 CFL 3377886 chr11 - 65347069 65386796 9.72 020238 005066 // PSF POMP100 2406064 014602 chr1 002898 SCR3 - 012154 35351696 3417583 35506894 9.80 chr12 + 55202025 55277435 9.78 NM_ // - NM_ // 001040694 NM_

45 NIP7 // MAN1A2 NM_ UCA1 HSPH1 NM_ SFPQ NM_ RBMS2EIF2C2 NM_ INCENP NM_ PIK3R4 NM_

50 kinase, kinase, 110kDa 110kDa 3- muscle) CFL1 NM_ rich 55 Gene NameGene Symbol Gene Accession Synonym nuclear import 7 homolog 7 homolog import nuclear cerevisiae) (S. epiregulin class alpha, mannosidase, // urothelial 2 member 1A, cancer EREG NM_ protein 1 protein heat shock 105kDa/ shock heat cofilin 1 (non- cofilin splicing factor proline/ factor splicing glutamlne- (polypyrimidine tract associated) protein binding phosphoinositlde- RNA binding motif, single stranded interacting protein 2 translation eukaryotic 2 2C, factor initiation protein centromere inner 135/155kDa antigens regulatory subunit 4, p150 4, subunit regulatory

59 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3331730 chr112778856 + chr4 58101868 - 58149782 9.54 99589201 99798839 9.53 3441849 chr12 - 6308185 6321522 9.60 2702307 chr33336422 - chr11 158305077 +3145020 158361233 9.60 chr8 66161951 66190547 - 9.60 95569109 95634851 9.57

30 I R- (continued) R // 5 R55 // R55 R // TNF- R // 6a 4 // TM4SF9 // // TM4SF9 4 //

35 // PR01073 001 FK5G11 // PZF // // PZF FK5G11 // HCNTF ZNF757 NET- TSPAN- CD120a // FPF // // FPF CD120a // TBP1 MGC19588 TNF- // // TNF- // // // TNFRI TNFAR TNFR55 // TNFR60 p55- // p55 // BM- ania- // DKFZp547K0918 // DKFZp547K0918 MGC75138 // LARK // RBM4A // // ZCCHC21 ZCRB3A // DKFZP4341.116 // DKFZp781B2117 // MGC138493 // MGC141940 MSTP054 40 053023 053023 000614 005723 015496 015496 001065 020307 002896 NM_ // NM_ // 170768 NM_ NM_ // NM_ 183009

45 TNFRSF1 ATNFRSF1 NM_ ZFP91 // // ZFP91 CNTF

55 Gene NameGene Symbol Gene Accession Synonym tetraspanin 5tetraspanin TSPAN5 NM_ tumor necrosis factor factor necrosis tumor receptor superfamily, 1A member cyclin L1 CCNL1 NM_ RNA binding motif protein 4 protein motif binding RNA RBM4 NM_ KIAA1429nucleoporin 153kDa 91 protein finger zinc // ciliary (mouse) homolog KIAA1429 NUP153neurotrophic factor NM 005124 N153 HNUP153 // 2943808 chr6 - 17723255 17855638 9.56

60 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2775463 chr43795942 - chr18 83492676 - 83515077 9.50 711592 803236 9.48 3405531 chrl23756262 + chr17 12856462 - 12874176 9.51 35881491 35911365 9.51 2593670 chr2 - 197962756 198039327 9.52 3315512 char11 + 197139 206202 9.52

30 (continued) YES yes

35 DBP // NRF2 // -NRF2 2588827 chr2 - 177794809 177837753 9.48 AUF1 // AUF1A // AUF1A // // AUF1 hnRNPD0 // P37 // P61- HsT441 // c- Yes // DKFZp5640176 // DKFZp5640176 E4- // FLJ30012 // HQ0256 // MSTP162 // DKFZP434F0318 // FLJ14950 CTEN PP14434 // PRP10 // // PRP10 PRPF10 // SF3b155 SAP155 MGC104517 // MGC104517 // MGC131931 // MQC148073 // MGC148074 synembryn // RIOS 40 182585 002138 005433 016355 016355 030817 032865 012433 021932 NM_ 006164// NM_ NM_ // 001003810 NM_ // NM_ NM // 031369 031370 NM_ // NM_ // 201224 NM_ NM_ // 001005526 NM_

45 NFE2L2 // // NFE2L2 DKFZp451M 2119 HNRPD YES1 NM_ DDX47 // APOLD1 RIC8A NM_ SF3B1 50 Asp) Asp) Ala- Glu-

55 Gene NameGene Symbol Gene Accession Synonym 1 Yamaguchi Yamaguchi 1 yes- v- (erythroid- factor nuclear // 2 2)-like derived protein hypothetical DKFZp451M2119 sarcoma viral oncogene oncogene viral sarcoma 1 homolog richelement RNA binding 37kDa) 1, protein tensin 4tensin nuclear heterogeneous D (AU- ribonucleoprotein TNS4 NM_ DEAD (Asp- box polypeptide 47 // 47 polypeptide box L domain apolipoprotein 1 containing resistance to inhibitors of of inhibitors to resistance A 8 homolog cholinesterase etegans) (C. 1, subunit 3b, factor splicing 155kDa

61 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3708826 chr17 + 7416768 7423040 9.46 2875555 chr5 - 132238768 132327205 9.38 2891052 chr5 -2570616 chr2 180596592 180612024 9.38 - 111088456 111174950 9.36

30 (continued) 4A // 4A // rs1 // H12.3 // // H12.3 rs1 35 // PIG21 7 // HRS // SRP40 // HRS 3542207 chr14 + 69263363 69308465 9.42 DDX2A // EIF- DDX2A // EIF4A // DKFZP586K0919 // DKFZp762A152 SSP3 // SMT3IP1 ADK2 2405364 chr1 - 33245959 33275155 9.45 - // FLJ23757- // // MCEF AF5Q31 2560254MGC75036 chr2 - 74607294 74610455 9.38 Gnb2- HLC- RACK1 // // BUB1L BUB1A hBUB1 40 001416 001416 001625 181575 181575 006925 015462 DKFZP586L0724 3732373 chr17 + 63144526 63205942 9.45 014423 006098 005871 // SPF30 SMNR 004336 3306516 chr10 - 112042540 112106248 9.38 NM_ // NM_ 015670 NM_ // NM_ 013411 NM_ // NM_ 133637 NM_ // 001039465 NM_

45 EIF4A1 // // EIF4A1 SENP3 AFF4 NM_ AUP1 // DQX1 SFRS5 SMNDC1 NM_ BUB1 NM_ GNB2L1 NM_

50 like 1 like

55 Gene NameGene Symbol Gene Accession Synonym rich 5 rich dependent ATPase) dependent ancient ubiquitous protein 1 protein ubiquitous ancient 1 polypeptide box DEAQ // (RNA- serine- nucleolar protein 11 protein nucleolar 2kinase adenylate NOL11 arginine/ factor, splicing AK2 NM_ eukaryotic translation translation eukaryotic isoform 4A, factor initiation // SUMO1/sentrin/SMT3 1 3 peptidase specific AF4/FMR2 family, member member family, AF4/FMR2 4 binding nucleotide guanine beta protein), (G protein 2- polypeptide survival motor neuron neuron motor survival 1 containing domain uninhibited budding BUB1 1 benzimidazoles by (yeast) homolog

62 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3429312 chr12 + 102848291 102871551 9.34 2609608 chr3 + 9414309 9495916 9.36

30 (continued)

35 ECGP // GP96 // GP96 // // ECGP - // // TRA1 GRP94 // GRP94P1 // HSP // // GRP94b // HSPCP2 // HsGrp94b TRAP1 // TRA1P1 DKFZp686J18276 DKFZp686J18276 // FLJ10707 // 1757 K1AA1 40 003299 003299 926615 926615 931417 931447 931478 944260 944280 944298 NM_ // NM_ // - 003211 XM_ XM_ // // 931376 XM_ XM_ // // 931444 XM_ XM_ 11 // 931455 XM_ XM_ // // 939712 XM_ XM_ // // 944276 XM_ XM_ // // 944295 XM_ XM_ // // 944303 NM_ 001080517

45 HSP90B1 // HSP90B1 // TDG HSP90B2P

55 // glycosylase DNA Gene NameGene Symbol Gene Accession Synonym heat shock protein 90kDa 90kDa protein shock heat // 1 member (Grp94), beta thymine- 90kDa protein shock heat 2 member (Grp94), beta (pseudogene) SET domain containing 5 containing domain SET SETD5

63 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2713074 chr3 - 198146677 198154763 9.23 2633773 chr33494137 chr13 + + 101910681 101950800 9.22 75092571 75566974 9.22 3646164 chr16 + 4415465 4446773 9.23 2417174 chr1 - 67646101 67669020 9.26 3773932 chr17 - 77091456 77105797 9.32

30 (continued) 1 35 // CHD3IP // 55 CBC2 // CBP20 // // CBP20 CBC2 // PIG55 NIP1 FLJ36137 // TF6 // TF6 // FLJ36137 TRKT3 // // FBX020 FBX20 LOMP // KIAA0858 CGI- // DKFZp564M2423 // FLJ90489 PAI- // HABP4L // PAIRBP1 RBP1 // // TID1 FLJ45758 hTid- MKP3 // MKP3 PYST1 3464860 chr12 - 88223376 88273467 9.31 ACT // ACTG // // // ACTG ACT DFNA26 // DFNA20

40 007362 005358 015047 RP1-43E13.1 2399620 chr1 - 19413665 19450633 9.22 015640 005147 001946 001946 014572 KPM // FLJ13161 3504526 chr13 - 20445178 20533718 9.28 001614 NM_ // 001007565 006070 NM NM_ // 001042540 NM_ NM_ // 001018067 NM_ // 001018068 NM_ // 001018069 NM_ NM_ // NM_ 022652

45 NCBP2 DNAJA3 NM_ LATS2 NM_ SERBP1 DUSP6

55 Gene NameGene Symbol Gene Accession Synonym fused gene fused TFG TRK- LIM domain 7KIAA0090 LMO7 KIAA0090 NM_ NM_ nuclear cap binding protein protein binding cap nuclear 2, 20kDa subunit DnaJ (Hsp40) homolog, 3 A, member subfamily LATS, large tumor 2 homolog suppressor, (Drosophila) SERPINE1 mRNA binding 1 protein actin, gamma 1 gamma actin, specificity dual 6 phosphatase ACTG1 NM_

64 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3556888 chr14 -2546008 chr2 22439714 224582312714955 9.18 - chr43237088 27718957 chr10 + 27740160 9.15 1692616 +2809628 1716693 17726140 chr5 9.12 177988093730899 9.11 + chr17 53849348 + 53878172 9.07 59204975 59250510 9.05

30 (continued) (gamma)

35 CAPERbeta // CAPERbeta // FLJ10482 PP239 // MGC4458 RNPC4 // // SR278 // FLJ37706 KLAA0764 // ART1 // MGC90306 // // // STAF65 SPT7L STAF65 // ERIC1 // MGC117382 MGC133242 // DKFZp686J2352 STAM1 // MGC150827 // MGC150829 // SH3PX2 // SH3PXD3B SNX18 // RHELP FLJ43179 RNAHP // // 40 007372 007372 018107 020207 014860 006342 003473 002531 NTR 052870 3892873 chr20 + 60810575 60864568 9.10 NM_ // NM_ 203499 NM_ // 001077351 NM_ // 001077352 NM_ // NM_ // 001034155 NM_

45 SUPT7L NM_ TACC3 NM_ STAMNTSR1 NM_ NM_ SNAG1 NM_ DDX42 RBM23 // // RBM23 C9orf102

50 Asp) Asp) Ala- Glu-

55 Gene NameGene Symbol Gene Accession Synonym suppressor of Ty 7 (S. Ty of suppressor cerevisiae)-like transforming, acidic coiled- 3 protein containing coil adaptor transducing signal and domain (SH3 molecule 1 motif) ITAM 1 receptor neurotensin affinity) (high associated nexin sorting 1 protein golgi DEAD (Asp- box polypeptide 42 polypeptide box RNA binding motif protein 9 open chromosome // 23 102 frame reading

65 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3599280 chr152823820 + chr5 65898917 66277975 + 9.03 110455769 110517812 9.03 3892607 chr203996667 + chrX 60305485 + 60317305 9.05 3891163 153644243 153659150 chr20 9.04 + 56848165 56919604 9.04

30 (continued) II //

35 DDXBP1 // GBP // // GBP DDXBP1 GU/RH- // MGC141878 // MGC141879 ZMIZ3 // DKFZp68611650 // TA- GLC1G TAWDRP WDRP // // GP110 // // GP110 // MGC29536 Rpn13 // NAP57 DKC // // XAP101 // NOLA4 dyskerin // C20orf45 // AHO // GPSA GNAS 1 GSP // GSA // // MGC33735 PHP1B // // PHP1A POH // dJ309F20.1.1 // dJ806M20.3.3 40 139281 007002 007002 000516 016592 080426 001363 016166 NM_ // NM_ 175573 NM_ // NM_ // 001077468 NM_ // 001077489 NM_ // 001077490 NM_ // NM_ // 080425 NM_ NR_ // 003259

45 DKC1 NM_ PIAS1 M_ ADRM1

55 Gene NameGene Symbol Gene Accession Synonym WD repeat domain 36 domain repeat WD WDR36 NM_ dyskeratosis congenita 1, 1, congenita dyskeratosis dyskerin GNAS complex locus GNAS of activated inhibitor protein 1 STAT, adhesion regulating regulating adhesion 1 molecule

66 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop + 359569 372958 8.99 Human Genome hg18 Genome Human

20 some Chromo Chromo chr1_ran chr1_ran dom

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 4041923 2975680 chr6 - 136619703 136652847 8.99 3049025 chr7 - 45103738 45128368 9.01 3666566 chr16 + 67722728 67761072 8.98 2624074 chr3 + 52694976 52705212 9.00 3326842 chr11 + 35600246 35826001 9.03

30 (continued) ISO // HLA- // HLA- ISO 6B // 35 ANIA- // DKFZp761A1210 // DKFZp7620195 HCLA- PCEE // ISO // AKIP AIP // // SB138 FLJ20608 // BTF // KIAA0164 // // KIAA0164 // BTF bK211L9.1 CPR2 // FASTKD4 // FASTKD4 CPR2 KIAA0948 // CIRHIN // CIRHIN // // FLJ14728 // // NAIC KIAA1988 TEX292 C77032 // E21G3 // // E21G3 // C77032 // NS MGC800 DIPB // HSA249128 DIPB // HSA249128 // MGC3490 MC7 // 40 030937 014739 014366 014366 004749 004749 199122 032830 017583 NM_ // 001039577 NM_ // NM_ 017900 NM_ // 001077440 NM_ // 001077441 NM_ NM_ // NM_ NM // 206825 206826 NM_ // NM_ // 030900 NM_

45 CCNL2 // AURKAIP1 CIRH1A NM_ BCLAF1 GNL3 TBRG4

50 containing 44 containing TRIM44 NM_

55 like 3 (nucleolar) 3 like Gene NameGene Symbol Gene Accession Synonym associated associated cyclin L2 // aurora kinase A kinase aurora L2 // cyclin interacting protein 1 guanine nucleotide binding binding nucleotide guanine protein- cirrhosis, autosomal (cirhin) 1A recessive BCL2- 1 factor transcription tripartite motif- tripartite transforming growth factor 4 regulator beta

67 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3283920 chr10 - 32134245 32261226 8.93 2391532 chr1 -2720181 chr4 1314609 1324575 + 8.96 17225344 17244808 8.95 3598959 chr15 + 65145043 65296818 8.97

30 (continued) ISO // HLA- // HLA- ISO 6B // 35 DKFZp779N2050 // DKFZp779N2050 // FLJ10971 // FLJ20737 // FLJ21785 FLJ45709 ANIA- // DKFZp761A1210 // DKFZp7620195 HCLA- PCEE // ISO // AKIP AIP // // SB138 FLJ20608 // // 1500003D12Rik // DKFZP434N185 // magicin EG1 DKFZP586N0721 // DKFZP586N0721 DKFZp686J10186 HSPC193// // JV15-2 // HsT17436 // MADH3 // // Smad MGC60396 3

40 030937 025205 005902 002799 Z 3225003 chr9 - 126155580 126223284 8.97 018287 NM_ // 001039577 NM_ // NM_ 017900

45 MED28 NM_ ARHGAP12 N_ PSMB7 NM_ CCNL2 // AURKAIP1

55 Gene NameGene Symbol Gene Accession Synonym mediator of RNA RNA of mediator II transcription, polymerase (S. homolog 28 subunit cerevisiae) Rho GTPase activating 12 protein SMAD family member 3 family SMAD SMAD3 (prosome, proteasome NM_ beta subunit, macropain) 7 type, A kinase aurora L2 // cyclin interacting protein 1

68 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2746024 chr4 + 146238626 146270126 8.86 3735107 chr17 + 711748013257938 71215729 chr10 8.86 + 93673509 93821994 8.84 2500919 chr22948425 + chr6 113117773 - 113137861 8.90 30676177 30694348 8.87 2360083 chr1 + 152459139 152510701 8.91

30 4 170 170 (continued) (II) 1 // PIT1 // PIT1 1 //

35 1 ABC38 // OABP // OABP // ABC38 // RNASEL1 RU // // RNS41 RNASELI // KLAA0940 // MGC138406 TAF // MOT1 DKFZp586L2022 // // DKFZp586L2022 HCNGP // HTRG // // // BSF3 HTRP CLC // // CISS2 // NR6 NNT1 // TAF172 // TAFII170 CAT53 // FB19 // FB19 // CAT53 PNUTS FLJ42300 // // FLJ42300 // NICE- KIAA0144 DKFZp686J2397 // // DKFZp686J2397 GLVR1 // FLJ41426 Glvr- // PiT-

40 013260 013260 002940 003972 002714 002811 S12 // P40 // MOV34 3668617 024321 chr16 - 014847 + 72888182 3830612 72901528 8.92 chr19 + 40811767 40820425 8.91 005415 NM_ // NM_ 013246 NM_ // 001040876 NM_

45 BTAF1 NM_ ABCE1 PPP1R10 NM_ // SAP30BP CLCF1 PSMD7 NM_ MGC10433 NM_ UBAP2L NM_ SLC20A1 NM_

50 like cytokine

55 Gene NameGene Symbol Gene Accession Synonym binding cassette,sub- ATPase, 7 (Mov34 (Mov34 7 ATPase, TFIID transcription factor- transcription TFIID like BTAF1 RNA polymerase II, polymerase RNA BTAF1 B- associated, 170kDa(Mot1 cerevisiae) S. homolog, ATP- family E (OABP), member 1 member E (OABP), family protein phosphatase 1, phosphatase protein (inhibitor) regulatory 10 subunit // protein binding SAP30 cardiotrophin- 1 factor proteasome (prosome, (prosome, proteasome subunit, 26S macropain) non- homolog) protein hypothetical MGC10433 protein associated ubiquitin 2- solute carrier family 20 20 family carrier solute transporter), (phosphate member 1

69 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2454532 chr1 - 210180312 210275613 8.81 3442205 chr12 - 6645924 6668961 8.79 2327482 chr1 + 28705062 28802493 8.81 2668351 chr3 - 33404835 33456874 8.80

30 I // (continued) 1a // 1a

35 1B // LBP- SED5 // STX5ASED5 3376193 // orf73 C1 chr11 // DKFZP434B168 INT7 - 62330946 62356126 8.84 CAGH1 CAGH1A // ERDA2 // CIZ // // NP // // NMP4 TNRC1 CHC1 // RCC1- // RNU17C U17HG // RNU17D A U17HG- // // DKFZp686L1745 LBP- LBP1A // LBP1B // LBP1A

40 001269 003164 001237 CCN1 // CCNA 015434 2784113 chr4 - 122956335 122964516 8.81 133476 014517 014319 MAN1 3420079 chr12 + 63806051 63928317 8.80 NM_ // 001048194 NM_ // 001048195 NM_ NR_ // 002909 XM_ // 001128716 NM_ NM_ // 001039916 NM_ // 001039917 NM_ // 001039918 NM_ // 001039919 NM_ // 001039920 NM_

45 INTS7 NM_ UBP1 NM_ RCC1 // SNHG3

55 Gene NameGene Symbol Gene Accession Synonym 1 a) protein coding) 3 cyclin A2 subunit complex integrator 7 of chromosome regulator CCNA2 small 1 // condensation gene host RNA nucleolar (non- NM_ LEM domain containing 3 containing domain LEM LEMD3 1 protein binding upstream (LBP- M_ syntaxin 5 STX5 zinc finger protein 384 protein finger zinc ZNF384

70 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2555490 chr2 - 61558490 61619343 8.71 3136129 chr8 - 57139946 571858913335089 8.72 chur11 + 64857703 64877276 8.71 2458701 chr13309215 chr10 - - 224398953 224463924 8.76 120621551 120830522 8.75

30 (continued) d4 BETA // BETA

35 eIF3- // p170 CRM1 // CRM1 // // DKFZp686B1823 ERBA- // // GRTH ERBA2 // MGC126109 // MGC126110 THR1 // // NR1A2 // THRB2 THRB1 REQ // MGC10180 ubi- UBID4 // // FLJ21967 // SPEC2FLJ21967 2828146 chr5 // FLJ27451 MGC102930 + 130616639 130781182 8.75 CAV // MGC12294 // CAV 3020273 chr7 GOCAP1 // GCP60 PAP7 GOLPH1 // // // EIF3A // EIF3 + // // P167 KIAA0139 eIF3- // // p180 p185 theta 115926553 115935830 8.78 40 003400 003400 006268 001233 001233 020240 00023 001101 PS1TP5BP1 022735 3036924 003750 chr7 - 5533433 5537011 8.77 NM_ // NM_ 000461 NM_ // NM_ 198212 NM_ // 001038702 NM_

45 DPF2 NM_ ZFAND2B 138802 NM - THRB XPO1 // 2528308 chr2 + 219779769 219782603 8.72 ACBD3 NM_ EIF3S10 NM_

50 type type

55 Gene NameGene Symbol Gene Accession Synonym erb- a) oncogene erb- a) oncogene Coenzyme A binding D4, zinc and double PHD PHD double and zinc D4, 2 family fingers zinc finger, AN1- finger, zinc 2B domain S20 protein ribosomal RPS20 homolog, (CRM1 1 exportin hormone thyroid // yeast) beta receptor, leukemia (erythroblastic NM_ (v- viral avian) 2, homolog actin, betaactin, acyl- 3 containing domain translation eukaryotic 10 subunit 3, factor initiation 150/170kDa theta, ACTB2 smallCDC42 effector NM_ CDC42SE2 caveolin 2 CAV2

71 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3331487 chr11 + 57235839 57391291 8.68 2435044 chr13448088 - chr123884892 149641830 - chr20 149753035 8.70 26141435 + 26179615 8.69 36968369 37015223 8.69 2522439 chr2 + 201384456 201418386 8.71

30 1 // (continued)

35 // 31 CGl- // DKFZp781O202 // MGC111151 // TMX2 // PIG26 CTNND // CAS // // KIAA0384 // P120CAS // p120 P120CTN KIAA0461 // // KIAA0461 // MGC71543 ZNF635 // SUHW5 SHARP- // DEC2 SHARP1 // C20orf129 // FLJ38341 dJ616B8.3 BZAP45 // BZAP45 // KIAA0005 Nbla10236 40 015959 015959 015100 015100 207171 030762 030919 014670 NM_ XM_ // // 001126721 XM_ // 001126756 XM_ // 001126767 XM_ // 001126781 XM_ // 001126793 XM_ // 001126823 001331 NM NM_ // NM_ // 145796 NM_ XM_ // 001126385 NM_

45 BHLHB3 NM_ FAM83D NM_ // TXNDC14 CTNND1 POGZ BZW1

50 helix helix loop- associated associated 55 Gene NameGene Symbol Gene Accession Synonym basic helix- basic B, class containing, domain 3 sequence with family D member 83, similarity domain thioredoxin // catenin 14 containing (cadherin- 1 delta protein), pogo transposable element element transposable pogo domain ZNF with basic leucine zipper and W2 W2 and zipper leucine basic 1 domains

72 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3303300 chr10 - 101938115 101979345 8.62 2987441 chr7 + 2315929 2386896 8.66 3398482 chr113151401 - chr8 130250320 130291615 - 8.67 124094605 124123781 8.67 3427767 chr12 + 97395927 97502543 8.68

30 (continued) alpha P116 // P116 3 // WIPI3 3 3775157 chr17 - 78165748 78199803 8.65 ETA // EIF3- // EIF3- ETA 35 // // DER1 1 IKBKA // IKK- // IKBKA // // IKKA IKK1 // 6 TCF1 // NFKBIKA EIF3- // EIF3- P110 // MGC104664 // MGC131875 eIF3b // PRT1 RBBP2 // RBP2RBBP2 3439603 // CHET8 // DKFZp667I205 chr12KIAA0254 DER- // FLJ13784 - // FLJ42092 // MGC3067 259504 368944 8.67 CMD1T // LAP2 // LAP2 // CMD1T // MGC61508 // TP PRO0868

40 001278 003751 019613 WIPI- 005056 014758 024295 NM_ // 001037283 NM_ NM_ // 001042603 NM_ NM_ // 001032283 NM_ // 001032284 003276 NM

45 CHUK NM_ DERL1 NM_ EIF3S9 JARID1A

50 helix loop-

55 like WDR45L NM_ Gene NameGene Symbol Gene Accession Synonym like domain family, family, domain like ubiquitous kinase ubiquitous WDR45- helix- conserved sorting nexin 19 nexin sorting Der1- member 1 SNX19 translation eukaryotic NM_ 9 3, subunit factor initiation 116kDa eta, jumonji, AT rich interactive interactive rich AT jumonji, 1A domain thymopoietin TMPO

73 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3974708 chrX + 40829542 40980776 8.57 3470253 chr12 - 107440140 107479296 8.57 3861978 chr19 -3243708 44568113 chr10 44592162 8.60 + 42597978 42682443 8.58 3599811 chr15 + 67493677 67527808 8.60 2427930 chr1 - 111782351 111793512 8.60

30 (continued) (nrb) 1 // - 1 // MKLP1 1 35 DFFRX // FAF // // FAF DFFRX AZFA // // AZF // SP3 DFFRY // KIAA0156 // MGC138188 RP11- 13G14// p110 // TIP110 FLJ11123 // PD2 // FLJ11123 // KNSL5 CHO1 // MKLP- // KIAA0187 // TTC7L1 c14_5685 HKMT1069 // HKMT1069 // MGC2722 MEP50 // Nubia10071 // // 552M11.3 RP11- // EGP // CHIT5 MUC9 // F23149 40 004856 004856 014753 004654 014706 006769 - 2345286 chr1 + 87458333 87588817 8.56 016133 MGC26273 2502424 chr2 + 118558758 118593436 8.57 024102 024102 019088 NM_ // NM_ 138555 NM_ // NM_ 001010854 NM_ // 001039590 NM_ // 001039591 NM_ NM_ // NM_ 002557

45 SART3 NM_ USP9X // USP9X // USP9Y BMS1L // // BMS1L TTC7B PAF1 NM_ WDR77 // WDR77 OVGP1

50 like,

55 Gene NameGene Symbol Gene Accession Synonym like, ribosome ribosome like, linked // ubiquitin ubiquitin // linked squamous cell carcinoma carcinoma cell squamous T by recognized antigen cells 3 LIM domain only 4 LMO4 NM_ kinesin family member 23 member family kinesin KIF23 2 gene induced insulin peptidase specific ubiquitin INSIG2 X- 9, Y- 9, peptidase specific (fat facets- linked NM_ BMS1- // (yeast) protein assembly repeat tetratricopeptide 7B domain Paf1, RNA polymerase II RNA polymerase Paf1, homolog factor, associated cerevisiae) (S. WD repeat domain 77 // 77 domain repeat WD 1, glycoprotein oviductal 120kDa (mucin 9, oviductin)

74 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3452323 chr12 - 45038242 45132603 8.50 2514441 chr2 +3512294 170149096 chr13 170206156 8.55 -3645253 chr16 43905532 44202063 +2491615 8.53 chr2 2742650 2761908 + 8.52 85597809 85625908 8.51

30 (continued) q // GAQ q // 3210808 chr9 - 79475043 79836455 8.53 Cyp // Cyp CYP // iso // XTP2 // iso 2367154 chr1 + 169716078 169829262 8.48

35 KD // ALPHA- VT // VT4VT // // KIAA1382 ATA2 // SAT2 PRO1068 3646434SNAT2 chr16 + 4836677 4872358 8.51 CARS- // MGC133241 DKFZp686019206 // MGC17597 // RP11- 269C23.2// // TSC22 TGFB114 300- DKFZp686015166 // FLJ21926 // // FLJ22250 // KIAA0324 // MGC40295 // SRm300 SRL300 // // MATII MATA2 SAMS2

40 016936 018976 015172 BAT2- 006022 006022 004792 002072 G- 016333 005911 NM_ // 001079514 NM_ NM_ // NM_ 183422

45 SLC38A2 NM_ GRPEL1 025196 NM HMGE // FLJ25609 2759404 chr4 - 7107908 7187815 8.48 PPIGGNAQ NM_ NM_ SRRM2 NM_ MAT2A NM_ TSC22D1

55 Gene NameGene Symbol Gene Accession Synonym arginine repetitive like 1, mitochondrial solute carrier family 38, 38, family carrier solute member 2 GrpE- (E. coli) 1containing domain BAT2 BAT2D1 NM_ peptidylprolyl isomerase G G isomerase peptidylprolyl G) (cyclophilin binding nucleotide guanine q protein), (G protein polypeptide serine/ 2 matrix methionine II, adenosyltransferase alpha 1ubinuclein UBN1 TSC22 domain family, family, domain TSC22 member 1

75 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3959631 chr222800503 - chr52436132 chr1 35236857 + 352554293502570 - 8.48 6736994 chr132772017 6893446 151900372 chr4 151910103 + 8.47 8.46 3149843 112999460 - chr8 113025981 8.45 688587002937984 - 68934802 chr6 8.45 1179098612423829 117956284 + 8.45 chr1 170705200 - 170723945 8.44 94409906 94549874 8.43

30 (continued) zeta // zeta B

35 // POLK 1 // MGC126526 // MGC126526 // eIF3- MGC17258 // eIF3- p66 eIF3d LAK- TRF4-1 // TRF4 // // NF45 MGC8391 PRO3063 CD107a // LAMPA// LGP120 YT521 // KIAA1966 YT521- // // FLJ25655 // // HR21 FLJ40596 HRAD21 KIA0078 // // // NXP1 MCD1 // // hHR21 SCC1 // GTF2D1 // GTF2D // MGC117320 // MGC126054 // MGC126055 TFIID // SCA17 // RP11- PARG1 255E17.1

40 33370 003753 006999 004515 207318 005561 3985866 006265 chrX + 003194 103297819 103323642 004815 8.45 NM_ // 001031732 NMJ_

45 EIF3S7 NM_ POLSILF2 NM_ CXorf39 NM_ LAMP1 NM_ NM_ RAD21 NM_ ARHGAP29 NM_

50 associated associated 55 Gene NameGene Symbol Gene Accession Synonym eukaryotic translation translation eukaryotic 7 3, subunit factor initiation 66/67kDa zeta, (DNA directed) polymerase sigma enhancer interleukin 2, 45kDa factor binding open X chromosome frame reading lysosomal- membrane protein1 YTH domain containing 1 YTHDC1 homolog (S. RAD21 pombe) protein binding box TATA TBPRho GTPase activating 29 protein NM_

76 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3712363 chr17 + 16886542 17062286 8.42 3185558 chr9 + 115077230 115095267 8.42 2673902 chr33886704 - chr203970166 49042148 + chrX 491064983851651 8.42 43028534 chr19 + 43142041 8.38 3351564 16714433 - chr11 16772561 8.36 12670912 + 12695776 8.35 117982385 118033939 8.34

30 (continued)

35 4 3665288 chr16 + 65783266 65790299 8.42 KIAA0864 // // KIAA0864 // p116Rip RHOIP3 HPRP4 // HPRP4P // HPRP4 Prp4p PRP4 // // FLJ20259 // // FLJ20259 MGC131838 // DKFZp686A2068 // // MST1 KRS2 YSK3 // FLJ11209 // FIAT // LSR5 // MGC126621 MGC126625 // // IPO3 FLJ12155 // TRN2 KPNB2B // DKFZp686H039 DKFZp686024210 // FLJ00141 // // FLJ90266 // // LL5A KIAA0638 MGC111531

40 015134 015134 001950 E2F- 017730 004697 000700 // LPC1 ANX1 006282 3174816 chr9 018360 + 013433 74914324 015157 74983394 8.41 NM_ // NM_ 201274 NM_ 198880 NM //

45 RIP // RIP E2F4 NM_ M- C17orf84 PRPF4 NM_ CXorf15 NM_ TNPO2 NM_ PHLDB1 NM_

50 Rho Rho like binding rich 1 QRICH1 mRNA 55 Gene NameGene Symbol Gene Accession Synonym threonine kinase 4 STK4 NM_ E2F transcription factor 4, p107/p130- glutamine- interacting protein interacting PRP4 pre- processing factor 4 (yeast) homolog phosphatase- myosin annexin A1annexin serine/ open X chromosome ANXA1 15 frame reading transportin 2 (importin 3, NM_ 2b) beta karyopherin homology- pleckstrin 1 member B, family domain,

77 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3655920 chr162378937 + chr1 29968869 +3154398 29991009 8.31 chr8 210275565 210399046 8.30 - 134535811 134653449 8.29 3684100 chr163836243 - chr19 21320984 + 22449842 8.33 50597660 50605831 8.33 3645555 chr16 + 3010334 3012380 8.34

30 (continued) 1 // 1 // CAST // CAST // 1

35 // NAc6S ALDA // MGC10942 MGC10942 // ALDA // MGC17716 // MGC17767 // // DCAF2 CDT2 L2DTL // RAMP Gal- // MGC9183 // // SIATFL SIAT4A // ST3GalA ST3GalA. DC49 // MLAS // MLAS // DC49 hLAT1-3TM // MMAA ASE- // MGC118851 PAF49 CD266 // FN14 // FN14 // CD266 TWEAKR 40 003033 003033 000034 000034 184043 016448 181847 DEGA // ALI1 3452478 chr12 030912 RNF27 // GERP - 3261820 45726359 chr10 45874177 8.30 + 104384137 104419190 8.29 012099 006845 MCAK // KNSL6 000574 2334098 TC // DAF // CR chr1 2377229 chr1 + 44978097 + 45005994 205561488 8.33 205607671 8.32 016639 002593 002593 NM_ // NM_ 173344 NM_ // NM_ // 184041 NM_ NR_ NR_ // 002594

45 DTLAMIGO2 NM_ NM_ ST3GAL1 ALDOA CD3EAP NM_ CD55 NM_ TNFRSF12A NM_ // LAT1-3TM IMAA

50 containing 8 containing TRIM8 NM_ sialyltransferase sialyltransferase 55 galactoside Gene NameGene Symbol Gene Accession Synonym 2,3- denticleless homolog homolog denticleless (Drosophila) Ig- with molecule adhesion 2 domain like beta- ST3 motif- tripartite alpha- 1 bisphosphate CD3e molecule, epsilon epsilon molecule, CD3e associated protein 2C member family kinesin KIF2C decay molecule, CD55 for factor accelerating blood (Cromer complement group) NM_ fructose- A, aldolase tumor necrosis factor factor necrosis tumor receptor superfamily, 12A member pseudogene SLC7A5

78 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3003193 chr7 + 56086894 56099148 8.22 2396480 chr1 -3083936 chr8 11049173 11082811 + 8.26 6553307 6633056 8.22 3283378 chr10 - 30511316 30764402 8.26

30 1 3377964 chr11 - 65407787 65412586 8.29 1- (continued) Scl- 2 // TCP- 2 zeta // CCT- CCT- // zeta 1 // CCT6 // // CCT6 1 //

35 PM/ // Scl AGPAT // LPAAT- // AGPAT CCT- zeta- Cctz // HTR3 // // HTR3 Cctz // MGC126214 // MGC126215 MoDP- zeta // TCP20 // // TCP20 zeta // TTCP20 TCPZ 100 // PMSCL // // // PMSCL 100 // RRP6 // PMSCL2 // p4 p3 // // p2 Rrp6p 1- epsilon // LPAAT- e PM- FLJ10486 // RP11- RP11- // FLJ10486 // // mtPAP 305E6.3 // // COLL6 CO11A1 STL2 FGF1BP // FIBP- // FGF1BP

40 001762 018361 002685 018109 018109 080629 004214 004214 NM_ // 001009186 NM_ NM_ // 001001998 NM_ NM_ // NM_ // 001854 NM_ 080630 NM // NM_ 198897 NM //

45 AGPAT5 NM_ CCT6A PAPD1 // PAPD1 // COL11A1 FIBP

50 like BCL9L 182557 NM // DLNB11 BCL9-2 3393993 chr11 - 118272076 118304947 8.23 phosphate phosphate 3- lymphoma 9- lymphoma 55 Gene NameGene Symbol Gene Accession Synonym acyltransferase 5 5 acyltransferase cell CLL/ acylglycerol- B- 1- O- acid (lysophosphatidic epsilon) acyltransferase, containing chaperonin 1) 6A (zeta subunit TCP1, exosome component 10 component exosome EXOSC10 PAP associated domain domain PAP associated collagen, 1 // containing 1 XI, alpha type fibroblast growth factor factor growth fibroblast binding intracellular (acidic) protein

79 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2409344 chr1 -2656738 chr3 43622176 43628144 + 8.20 187961636 187990742 8.20 3090006 chr8 +3948461 chr22 23439117 23485313 + 8.21 43938390 43960160 8.21 2451309 chr1 - 200963111 201048571 8.22

30 1 (continued)

35 // // DDX2B 010 ARC32 // ARC32 // MGC17544 MGC19641 BM- EIF4F // EIF4A HT015 // MFRN // // MFRN HT015 MSCP // MSC // // PRO1278 // PRO1584 PRO2217 // MGC39961 // NPAP60 NPAP60L FLJ10538 // // FLJ10538 // FLJ12459 // FLJ12491 // FLJ16281 PLU- // FLJ23670 // PUT1 // RBBP2H1A

40 153645 052877 007172 007172 001967 016612 006618 NM_ // 001001651 NM_ // 001001653 NM_ // 001001654 NM_ // NM_ 201542 NM_ // M_ XM_ // 001128238 XM_ // 001128248 XM_ // 001128255 XM_ // 001128269 NM_

45 EIF4A2 NM_ MED8 JARID1B NM_ SLC25A37

55 Gene NameGene Symbol Gene Accession Synonym eukaryotic translation translation eukaryotic initiationfactor 4A, isoform 2 nucleoporin 50kDanucleoporin NUP50 RNA of mediator II transcription, polymerase (S. 8 homolog subunit cerevisiae) jumonji, AT rich interactive interactive rich AT jumonji, 1B domain 25, family carrier solute 37 member

80 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3623683 chr152881521 - chr53304012 48356681 48434794 chr10 - 8.18 - 150050460 1500608852921086 8.16 103534201 chr6 103568420 8.15 +2409104 chr1 110606544 110682171 8.13 - 43124794 43338329 8.12

30 (continued)

35 BABPB2 // E4TF1 // E4TF1 // BABPB2 // E4TF1- E4TF1-47 // E4TF1B // 53 GABPB // GABPB1 // NRF2B1 // // FLJ10290 ZC3H16 // FLJ11229 // FLJ23355 MEA5 // KIAA0679 NCOAT // // FLJ10564 // EHB3 // MGC102802 PRPF17 // PRP17 // // GLUT1 GLUT // MGC141895 MGC141896

40 002041 002041 016654 181427 018047 012215 000527// FHC FH 015891 3821015 016391 chr19 HSPC185 006516 + 2888284 11061114 chr5 11115050 8.15 - 175743557 175749348 8.13 NM_ // NM_ // 005254 NM_ // NM_ // 016655 NM_

45 RBM22 NM_ MGEA5 NM_ LDLRCDC40 NM_ HSPC111 NM_ NM_ SLC2A1 NM_ GABPB2

55 Gene NameGene Symbol Gene Accession Synonym RNA binding motif protein 22 expressed meningioma 5 (hyaluronidase) antigen lipoprotein density low receptor hypercholesterolemia) cycle division cell (familial (S. cerevisiae) homolog 40 protein hypothetical HSPC111 2 family carrier solute glucose (facilitated transporter), member 1 GA binding protein protein binding GA beta factor, transcription 2 subunit

81 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3147020 chr82555630 - chr2 102226101 102376609 - 8.08 61939693 61970469 8.07 3029030 chr73559570 + chr143600744 142695524 - 142714904 chr15 8.11 30629936 + 310023643200611 8.10 70553731 chr9 70666726 8.09 - 19042752 19093153 8.09

30 (continued) 1L // 1L 113 1S // ICH1 // ICH1 // 1S 2 // ICH- // 2 79 3990795 chrX + 129356824 129381607 8.09 35 1L/ HSPC038 // PNAS- HSPC038 // PNAS- 106 // Cctd MGC126164 // MGC126165 // SRB CASP- ICH- NEDD2 // FLJ38315 KIAA1131 // HARI ARI HHARI // UBCH7BP // MGC102696 // MGC138798 // MGC138799 RP11- 296P7.3

40 032982 032982 016096 006430 015382 005744 016024 CGI- 017645 005966 - 2520225 chr2 + 191205069 191437200 8.08 NM_ // NM_ 032983 NM_ // 001042510 NM_ // 001042511 NM_

45 CCT4 NM_ CASP2 ARIH1RBMX2 NM_ NM_ FAM29A NM_ NAB1 NM_

55 Gene NameGene Symbol Gene Accession Synonym A binding protein 1 1 protein A binding linked 2 linked chaperonin containing containing chaperonin 4 (delta) subunit TCP1, caspase 2, apoptosis- 2, caspase related cysteine peptidase peptidase cysteine related cell precursor (neural expressed, down- developmentally 2) regulated HECT domain containing 1 HECTD1 ubiquitin- homolog, ariadne E2 enzyme conjugating 1 protein, binding NM_ (Drosophila) RNA binding motif protein, X- sequence with family A member 29, similarity NGFI- 1) protein binding (EGR1 706 protein finger zinc ZNF706

82 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3595096 chr15 + 54963208 55402126 8.03 3577277 chr143752424 - chr17 92773656 - 92966460 8.05 27203014 27210424 8.04 3730211 chr17 + 57854988 57881176 8.06

30 (continued) 1 3125775 chr8 - 17128912 17148758 8.05

35 HEB // HTF4 // HTF4 HEB // HsT17266 DKFZp686N0544 // DKFZp686N0544 FUP1 // MGC48310 // FLJ21119 // HSA272196 TTP1 CAF1 // hCAF- // CAF1 FLJ11350 // // FLJ11350 // // METL FLJ12760 // METTL2 // METTL2A PSENIP1 40 003205 003205 207037 207040 018167 018405 013354 013354 004592 SWAP 3438417 chr12 + 130761587 130852472 8.05 018396 018396 181725 022452 // FLJ11618 FBS 3656362 chr16 + 30577810 30590035 8.06 017612 DKFZp434E2220 3475679 chr12 - 121522105 121551469 8.07 NM_ // NM_ // 207036 NM_ // NM_ // 207038 NM_ NM_ // 001002860 NM_ NM_ 054026 NM // NM_ // NM_ // 001005372 NM_

45 C17orf79 NM_ TCF12 BTBD7 CNOT7 SFRS8 NM_ ZCCHC8 NM_ // METTL2B METTL2A

50 helix helix loop-

55 homolog, apricot Gene NameGene Symbol Gene Accession Synonym NOT transcription transcription NOT rich 8 (suppressor- rich white- chromosome 17 open 79 frame reading 12 factor transcription helix- (HTF4, 4) factors transcription BTB (POZ) domain BTB (POZ) domain 7 containing CCR4- 7 subunit complex, Drosophila) of- serine- fibrosin 1fibrosin arginine/ factor, splicing FBS1 NM_ zinc finger, CCHC domainzinc finger, containing // 2B like methyltransferase 2A like methyltransferase

83 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3653398 chr16 + 24583665 24748478 7.98 2709062 chr3 - 187048509 187160523 7.98 2358171 chr13680610 chr16 +3883787 148560583 - chr20 148592321 8.03 3690084 11865619 + 11917408 chr16 8.00 34287657 - 34322234 7.99 45546783 45565155 7.98

30 (continued) beta // // beta

35 // 23 CAGH26 // CAGH26 // DKFZp666E117 // // GW1 FLJ22043 // GW182 // KIAA1460 // MGC75384 TNRC6 DKFZp686F18120 DKFZp686F18120 Htra2- // TRA2- // SRFS10 // TRA2B BETA HPRP3 // HPRP3P // HPRP3 // Prp3p PRP3 // // // // FLJ32145 RP18 HSPC099 // ETF3A 551G9.2 // eRF3a GST1 CGI- // DKFZp564N1363 bA234K24.2 // // DJA2 CPR3 DNAJ // DNJ3 // PRO3015 // HIRIP4 RDJ2 // 40 020847 020847 004698 004698 004593 002094 024741 FLJ12827 015511 3329461 005880 chr11 + 46678944 46684037 7.99 018066 FLJ10349 2402838 chr1 - 27073870 27089311 8.03 NM_ // NM_ 014494 NM_ // NM_ 015203

45 TNRC6A SFRS10 NM_ C20orf4 NM_ DNAJA2 NM_ ATPBD18 NM_ PRPF3 // KIAA0460

50 mRNA 55 Gene NameGene Symbol Gene Accession Synonym rich 10 (transformer (transformer 10 rich trinucleotide repeat repeat trinucleotide 6A containing serine- Drosophila) homolog, 2 G1 to S phase transition 1 transition S phase to G1 GSPT1 408 protein finger zinc chromosome 20 open ZNF408 NM_ 4 frame reading NM_ DnaJ (Hsp40) homolog, 2 A, member subfamily arginine/ factor, splicing ATP binding domain 1 domain binding ATP B member family, PRP3 pre- processing factor 3 // (S. cerevisiae) homolog KIAA0460

84 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2880932 chr5 - 148800168 148922811 7.96 3929395 chr21 - 33028084 33066030 7.96 3203582 chr9 - 33442676 33464087 7.96 3217807 chr93260666 - chr103626826 102104197 + chr15 1021554713976299 7.98 102279093 chrX - 102303662 7.97 57215720 + 57452363 47300826 7.97 47316249 7.96

30 (continued) IC // IC //

35 // 020 RAF // ARAF1 // // ARAF1 RAF CK1 // HLCDGP1 // HLCDGP1 // // CK1 PRO2975 BM- GCFC // FLJ90561 FLJ21959 // // FLJ21959 // MGC14896 // MGC14921 // MGC20838 // UTP22 NRAP // bA311H10.1 FLJ20287 // // FLJ20287 bA208F1.2 // DKFZp762F1811 // FLJ20615 // FIH1 FLJ22027 HuncM- // MGC104638 MYO1C A- // RAFT1 PKS2 40 018410 hFLEG1 2604254 chr2 - 234406876 234427931 7.95 001892 145328 145328 016631 130793 130793 139235 017746 020401 NUP84 017902 004998 3421177 chr12 001654 + 67366998 67423025 7.97 NM_ NM_ // 001025105 NM_ NM_ // NM_ // 013329 NM_ // NM_ 058191 NM_ // NM_ // 022917 NM_

45 DKFZp762E1 DKFZp762E1 312 C21 orf66 C21 TEX10 NM_ HIF1AN NM_ ARAF NM_ NOL6

55 1, factor inducible Gene NameGene Symbol Gene Accession Synonym associated) raf murine sarcoma 3611 3611 sarcoma murine raf hypothetical protein protein hypothetical DKFZp762E1312 casein kinase 1, alpha 11, alpha kinase casein CSNK1A1 chromosome 21 open 66 frame reading testis expressed sequence sequence expressed testis 10 107kDanucleoporin hypoxia- inhibitor subunit alpha NUP107myosin IE NM_ v- homolog oncogene viral 6 family protein nucleolar MYO1E(RNA- NM_

85 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3240340 chr10 +2982381 28828043 chr6 29005095 7.92 - 160119521 160130731 7.92 3961496 chr22 - 39136248 39362660 7.93 3893849 chr20 + 62082901 62134891 7.95

30 (continued) alpha 1- A alpha // CCT1 CCT1 // alpha 1 // C20orf14 // C20orf14 1 //

35 // 016 CCT- D6S230E // CCTa // TCP- // BM- // MGC10753 // Wwp4 PRO1741 // bA48B24 // FLJ22858 3601741 chr15 + 72677906 72719105 7.91 - // // MAL BSAC MRTF- 3874438 chr20 + 3715655 3734756 7.93 ANT- // U5-102K // TOM hPrp6 40 030752 001292 016628 016628 100486 025090 DUB1 002721 3772581 - chr17 - 3225348 74295075 chr9 74348574 7.92 - 126948675 126991992 7.91 004358 004358 021873 020831 012469 005706 - 3317338 chr11 + 2378304 2381662 7.93 NM_ // 001008897 NM_ NM_ // NM_ 003992 NM_ // NM_ // 100264 NM_ NM_ // NM_ // 021872 NM_

45 USP36 NM_ PPP6C NM_ MKL1 TOP1 NM_ WAC PRPF6 NM_ TSSC4 NM_ CDC25B

50 coil mRNA 55 Gene NameGene Symbol Gene Accession Synonym like kinase 3 kinase like CLK3 complex 1 TCP1 ubiquitin specific peptidase peptidase specific ubiquitin 36 t- 6, phosphatase protein catalytic subunit CDC- megakaryoblastic leukemia leukemia megakaryoblastic 1 (translocation) I (DNA) topoisomerase TOP1 containing domain WW coiled- with adaptor 003286 NM TOPI 3885464 chr20 + 39090891 39186535 7.93 PRP6 pre- processing factor 6 (S. cerevisiae) homolog suppressing tumor candidate subtransferable 4 25 cycle division cell pombe) B (S. homolog

86 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2949038 chr6 - 31605990 31622606 7.87 2440625 chr1 - 159357395 159369167 7.89 2921296 chr63086206 chr8 +2581548 111287588 chr2 + 111324441 7.90 11690497 - 11740987 7.90 153212414 153283546 7.89 2997376 chr7 + 36395957 36462017 7.90

30 (continued) REN- 6

35 // // FBP11 11 D6S81E // DDX39B // DDX39B D6S81E // ATP6G UAP56 // // NG38 ATP6G2 // VMA10 // HZFP100 // ZN473HZFP100 3839142 chr19 + 55220811 55248476 7.87 CASP8IP1 // // CASP8IP1 // // DEFT DEDD1 KE05 // FLDED1 FBP- FLJ20585 // FLAF1 HIP10 // FNBP3 // // HYPA // NY- ADOMETDC // ADOMETDC // AMD // DKFZp313L1234 FLJ26964 // ERG9 // DGPT SS SQS // ANILLIN // // ANILLIN // DKFZp779A055 scra // Scraps 40 004640 004640 130463 015428 032998 001634 004462 018685 371575 371575 NM_ // NM_ // 080598 NM_ // NM_ 138282 NM_ // 001006656 NM_ XM_ XM_ // 938514 NM_ // 001039711 NM_ // 001039712 NM_ NM_ // 001033059 NM_

45 BAT1 // ATP6V1G2 FDFT1 NM_ PRPF40A DEDD AMD1

50 mRNA

55 diphosphate Gene NameGene Symbol Gene Accession Synonym B associated associated B HLA- H+ // ATPase, 1 transcript lysosomal transporting, 13kDa, V1subunit G2 integrin, beta 6 beta integrin, 473 protein finger zinc ZNF473 ITGB6 000888 NM - 2583465 chr2 - 160664438 160818586 7.88 famesyl- 1 farnesyltransferase pre- PRP40 processing factor 40 cerevisiae) A (S. homolog domain effector death containing anillin, actin binding protein binding actin anillin, ANLN adenosylmethionine 1 decarboxylase NM_

87 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3952637 chr22 - 17696576 17799452 7.82 3282213 chr103765689 - chr17 27439066 - 27484191 7.84 57374750 57498031 7.84 3894228 chr203261447 - chr10 402069 + 472534 103882745 7.87 103900072 7.86

30 (continued)

35 -// TUP1 // DGCR1 TUPLE1 3056108 chr7 - 72588624 72610244 7.82 FTSH // MEG4 // // // MEG4 FTSH YME1L // PAMP DRIP250 // ARC250 // HSPC221 // // KIAA0593 TRAP240 // MED13 CK2A1 // CKII // CKII // // CK2A1 // - alpha CKII // KIAA0595 PRC // MGC74642 RP11-302K17.6 // 40 77559 001707 001707 003325 001895 001895 014263 139313 005121 017798 // C20orf21 3913712 chr20 - 61297230 61330873 7.83 015062 002207 NM_ // NM_ 138707 NM_ // NM_ // NM_ // 177560 NR_ NM_ // NM_ // 139312 NM_

45 HIRA NM_ THRAP1 NM_ YTHDF1 NM_ PPRC1 NM_ CSNK2A1 // CSNK2A1P

50 related 1 related lymphoma 7B lymphoma BCL7B 55 Gene NameGene Symbol Gene Accession Synonym like(S. 1 cerevisiae) YME1L1 cell CLL/ HIR histone cell cycle cycle cell histone HIR defective regulation A (S. cerevisiae) homology thyroid hormone receptor receptor hormone thyroid 1 protein associated family, YTH domain member 1 B- peroxisome proliferator- peroxisome gamma, receptor activated coactivator- YME1- casein kinase 2, alpha 1 1 2, alpha kinase casein kinase // casein polypeptide 1 polypeptide alpha 2, pseudogene

88 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3377752 chr11 - 65121806 65139693 7.77 2830010 chr5 +3002640 chr7 135464462 135552314 7.77 + 55054070 55291773 7.77 2524577 chr2 + 206732303 206735884 7.78 3386814 chr113231774 - chr10 93102831 93114308 + 7.81 942450 1055862 7.79

30 (continued)

35 MGC17114 // MLK- // MGC17114 // PTK1 // MLK3 // 3 SPRK DKFZp781C1895 // DKFZp781C1895 // DKFZp78101323 // JV5-1 // Dwfc MADH5 // // ERBB1 ERBB mENA EEF1B // EEF1B EEF1B1 EF1B MGC5306 // ACA25 ACA25 // MGC5306 // ACA18 ACA32 // FLJ10686 // CRFG // FLJ10690 // NGB // FLJ39774 40 005228 005228 201283 002419 005903 001959 024116 024116 012341 003032 003032 NM_ // NM_ // 201282 NM_ // NM_ 201284 NM_ // 001001419 NM_ // 001001420 NM_ NM_ // 001037663 NM_ // NM_ 021121 NM_ NR_ // // 003028 NR_ NR_ // 002959

45 MAP3K11 NM_ EGFR EEF1B2 JOSD3 // JOSD3 // SNORA25 // SNORA32 SNORA18

50 erb- b)

55 protein activated Gene NameGene Symbol Gene Accession Synonym kinase kinase kinase 11 kinase kinase kinase epidermal growth factor factor growth epidermal (erythroblastic receptor (v- viral leukemia mitogen- oncogene homolog, avian) homolog, oncogene SMAD family member 5 family SMAD SMAD5 GTP binding protein 4 protein GTP binding GTPBP4 translation eukaryotic 2 1 beta factor elongation NM_ Josephin domain domain Josephin small 3 // containing box H/ACA RNA, nucleolar RNA, nucleolar small // 25 H/ACA box 32 // small H/ACA RNA, nucleolar

89 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3751184 chr172407163 - chr13334224 24256404 - chr11 24302905 7.73 37774050 + 37792490 7.72 63709341 63728586 7.71 3729294 chr173996404 + chrX 55325239 55429105 + 7.73 153318480 153324978 7.73 3327906 chr113687715 + chr16 43290109 43322649 - 7.77 30275789 30289100 7.74

30 (continued) SSP- alpha

35 // AAC11 // 11 PS6K // S6K // S6K1 // S6K1 // S6K PS6K p70 // STK14A // // p70- (S6K)-alpha // p70- S6K // KIAA1523 // PF1 MGC131914 RP3- // FLJ12553 // 423B22.3 dJ423B22.2 IEF- // HOP L STI1 // P60 // 3521 FLJ41411 // GDIL // // GDIL FLJ41411 // MRX48 // MRX41 OPHN2 // RABGD1A // XAP- RABGDIA // AAC- API5L1 // DKFZP434P1750 FP2461

40 015934 HSPC120 003161 2523144 chr2 + 202811346 202926967 024700 7.73 006819 001493 006595 017812 FLJ20420 015527 3073597 chr7 - 132062426 132500566 7.75 NM_ // 001033561 020889 NM NM_

45 RPS6KB1 NM_ SNIP1 NM_ STIP1 NM_ CHCHD3TBC1D10B NM_ NOP5/NOP5 NM_ 8

50 coil- coiled- organizing organizing helix- 55 Gene NameGene Symbol Gene Accession Synonym induced- coil- ribosomal protein S6 protein ribosomal polypeptide 70kDa, kinase, 1 interacting nuclear Smad 1 protein stress- 1 phosphoprotein (Hsp70/Hsp90- protein) GDP dissociationinhibitor 1 GDI1 12 protein finger PHD NM_ PHF12 apoptosis inhibitor 5 inhibitor apoptosis coiled- 3 containing domain helix API5 family, domain TBC1 10B member protein nucleolar NM_ NOP5/NOP58

90 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3714729 chr17 + 21128581 21159113 7.70 2960903 chr6 - 74281167 74335800 7.70

30 (continued) 16303 16303 1 3 // CCS3 // // CCS3 3 35 // EEF1A 1 // Tu // EF1A // EF1A Tu // MAPKK3 // MEK3 // MEK3 MAPKK3 // // PRKMK3 MKK3 TEF2 3761905CCS- EEF- chr17EF- GRAF- // FLJ25721 // HNGC: 1EF - // LENG7 // // MGC102687 // MGC131894 45031245 PTI1 // MGC16224 eEF1A- // 45110541 7.71

40 145110 145110 145109 003563 001402 XM_ // 001130488 NM_ // NM_ // 002756 NM_ NM_ // 001007226 NM_ // 001007227 NM_ // 001007228 NM_ // 001007229 NM_ // 001007230 NM_

45 EEF1A1 NM_ MAP2K3

50 activated protein protein activated

55 protein POZ type SPOP Gene NameGene Symbol Gene Accession Synonym eukaryotic translation translation eukaryotic 1 1 alpha factor elongation kinase kinase 3 kinase kinase mitogen- speckle-

91 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2566740 chr22693081 - chr3 99301923 - 99319337 7.69 126427204 126577074 7.69 3151534 chr82326954 - chr12622469 124393174 chr3 124477871 + 7.69 27521221 + 27535639 7.69 50101372 50134000 7.69

30 (continued) 4 1 // BFCOL1 BFCOL1 1 // 35 BETA // ZBP- APACD // LYGH // // LYGH APACD // // MGC119046 // MGC119047 MGC119049 BERF- HT- // 89 // ZFP148 // pHZ- 52 FLJ33908 // MrDb // // MrDb FLJ33908 2502300 // DKFZp667N1320 chr2 // MGC131938 // MGC142216 // MGC29843 + // MGC5254 // DKFZP564D0478 // MGC111002 118243834RP11- 4K3 A. 118323562// G15 // FLJ39876 7.70 // LUCA15 // H37 RMB5 40 005783 005783 006773 006773 021964 003749 - 3525234 chr13 - 109196024 109238228 7.68 014109 032125 005778 NM_ // NM_ 175735 NM_ // NM_ 003393

45 TXNDC9 // TXNDC9 // LYG2 ATAD2 NM_ C1orf160 NM_ DDX18 // WNT8B 50 Asp) Asp) Ala- Glu-

55 MMTV type Gene NameGene Symbol Gene Accession Synonym zinc finger protein 148 protein finger zinc 48 ZNF 2 substrate receptor insulin IRS2 NM_ NM_ like ATPase family, AAA family, ATPase 2 containing domain open 1 chromosome 160 frame reading 5 protein motif binding RNA RBM5 domain thioredoxin lysozyme- 9 // containing NM_ DEAD (Asp- family, site integration box polypeptide 18 // 18 polypeptide box wingless-

92 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2346934 chr1 + 93147511 93377202 7.63 3980887 chrX + 70420006 70437726 7.64 3706071 chr17 + 1874907 1895099 7.64 3820663 chr19 +2964200 chr6 10625547 10664074 7.68 - 90093065 90119338 7.66

30 (continued) AT- 90 90 AT- 1 // TCP80 // 1

35 // HSPC153 76 M96 // PCL2 // // // PCL2 M96 // RP5-976013.1 dJ976O13.2 FLJ12796 2354082 chr1 + 118273827 118304572 7.63 KIAA0138 3847252 chr19 - 5533105 5575015 7.64 NMT55 // NRB54 // // NRB54 // NMT55 P54NRB // P54 DPH2L // DPH2L1 // DPH2L1 // DPH2L // FLJ33211 //- OVCA1 DRBF // DRBP76 // // // DRBP76 DRBF // MMP4 // MPHOSPH4 // MPP4 NF- // // NFAR NF90 // NFAR- GTT1 2565143 chr2 - 96214334 96238296 7.65 CGI- // HSPC205 // // HSU93243 // MGC12555 // Ubc6pNCUBE1 40 001383 001383 020151 020151 004516 004516 153464 016021 I NM_ 007368 I NM_ 006784 I NM_ 014649 I NM_ 007363 NM_ // NM_ 060822 NM_ // NM_ 139267 NM_ // NM_ // 012218 NM_

45 MTF2 SAFB2 NONO DPH1 // DPH1 // OVCA2 UBE2J1 NM_ STARD7 ILF3

55 conjugating Gene NameGene Symbol Gene Accession Synonym POU domain POU domain metal response element element response metal factor transcription binding 2 WD repeat domain 3 domain repeat WD WDR3 scaffold attachment factor factor attachment scaffold 82 non- octamer- containing, binding DPH1 homolog (S. (S. homolog DPH1 candidate // cerevisiae) tumor suppressorovarian in 2 cancer ubiquitin- (UBC6 J1 E2, enzyme yeast) homolog, containing domain START 7 interleukin enhancer enhancer interleukin 3, 90kDa factor binding

93 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3362719 chr11 -3633403 chr15 104875742765590 10788746 - chr4 7.60 3464747 73448786 chr12 - 73535167 7.60 - 35626248 35922356 87349442 7.60 87498371 7.58 2954646 chr6 - 43587500 43592701 7.61 2545681 chr23361116 - chr11 27402231 27433372 - 7.63 6657673 6690484 7.62

30 (continued) L26 // RPL17L // RPL17L L26 35 1 // Kitl // MGF // // MGF // 1 // Kitl AAG1 // DAP5 // // DAP5 AAG1 // NAT1 FLJ41344 p97 // DKFZP434K2235 // FLJ90319 KIAA0700 FLJ13675 // ARAP2 // FLJ4-0916 // PARX // KIAA0580 // DKFZp686F2250 KL- // SF SCF C6orf109 // // C6orf109 // DKFZP566C243 // KLIP1 // FinGER3 dJ337H4.3 // // FLJ44836 // MGC131686 dJ337H4.2 KIAA0011 // TFIIIC- KIAA0011 // TFIIIC110 BETA MRP- RPML26 // 40 015230 015230 000899 001418 007067// HBOA HBO1 015477 3725779 chr17 + 45196447 45261455 7.60 015388 015388 001521 005316 TFIIH // BTF2 022061 3322717 chr11 + 18300412 18345156 7.62 NM_ // NM_ 139182 NM_ // NM_ 003994 NM_ // 001042559 NM_ NM_ // NM_ 001012974 NM_ // 001035521 NM_

45 MYST2SIN3A NM_ NM_ EIF4G2 GTF2H1MRPL17 NM_ NM_ // YIPF3 C6orf154 GTF3C2

55 Gene NameGene Symbol Gene Accession Synonym MYST histone histone MYST 2 acetyltransferase A, homolog SIN3 regulator transcription (yeast) 1 delta centaurin, ligandKIT CENTD1 KITLG eukaryotic translation translation eukaryotic 2 gamma, 4 factor initiation general transcription factor factor transcription general 62kDa 1, polypeptide IIH, ribosomal mitochondrial L17 protein family, domain Yip1 6 chromosome // 3 member 154 frame reading open general transcription factor factor transcription general beta 2, polypeptide IIIC, 110kDa

94 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3903836 chr203309755 - chr10 33276003 33336225 - 7.55 121568302 121642742 7.55 3778601 chr18 + 9903984 9950012 7.56 3057755 chr7 - 76037679 76196100 7.56 3336696 chr11 + 66643299 66782124 7.57

30 33 (continued) A //

35 // p27BBP gcn (2) FLJ13081 // // FLJ13081 FLJ36756 CAB // EIF3A // EIF6 // EIF6 CAB // EIF3A b // MGC3745 // VAP- // MGC3745 VAP- // 33 hVAP- // VAP33 MGC8359 // POM- POM- // MGC8359 POM121 // ZP3 CXXC8 // CXXC8 DKFZP434M1735 // FBL7 // FBL11 // // FLJ00115 // FLJ46431 // JHDM1A LILINA // KIAA1004 40 024834 018195 FLJ10726 3348891 chr11 + 111450087 111461067 7.54 002212 002212 181467 181469 003574 003574 012230 012230 012308 NM_ // NM_ // 181466 NM_ // NM_ 181468// NM_ NM_ // NM_ 194434 NM_ // NM_ 152992

45 C10orf119 NM_ C11orf57 NM_ ITGB4BP VAPA POMZP3 FBXL11 NM_

50 rich rich associated associated

55 Gene NameGene Symbol Gene Accession Synonym box and leucine- and box chromosome 10 open 119 frame reading chromosome 11 open 57 frame reading integrin beta 4 binding binding 4 beta integrin protein VAMP (vesicle- VAMP membrane protein protein)-associated A, 33kDa POM (POM121 homolog, homolog, (POM121 POM fusion ZP3 and rat) repeat protein 11 protein repeat F-

95 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3580179 chr14 - 1016168422762468 101676327 7.53 chr4 -3440598 chr12 17404173 17421482 - 7.53 2836207 2856564 7.52

30 1 // 1 (continued) 3 // INS- 3 // 11 // HFH11 HFH11 // 11 35 // // MPP2 2 FKHL16 // FOXM1B FOXM1B // FKHL16 HFH- // HNF- // FLJ31884 // HSP86 // HSP86 FLJ31884 // HSP90A // HSPC1 // HSP90N HSPCA // // // HSPCAL1 HSPN // HSPCAL4 // // Hsp90 Hsp89 // // LAP2 // HSP90ALPHA // HSPCAL3 // FLJ20280 // MGC126765 MGC126767 // MPHOSPH2 MPP- TRIDENT // PIG29

40 005348 021953 202003 000319PXR1 // PTS1R 017741 3403299 chr12 + 7232607 7262437 7.53 NM_ // 001017963 NM_ // NM_ // 001040141 - NM_ // NM_ // 202002 NM_

45 PEX5C4orf30 NM_ NM_ HSP90AA1 // HSP90AA1 // HSP90AA2 HSP90AA6P

55 Gene NameGene Symbol Gene Accession Synonym peroxisomal biogenesis biogenesis peroxisomal 5 factor open 4 chromosome 30 frame reading 2 protein transmembrane TMEM2 M1 box forkhead 013390 NM - FOXM1 3209384 chr9 - 73452177 73573229 7.52 heat shock protein 90kDa 90kDa protein shock heat A class (cytosolic), alpha shock heat 1 // member alpha 90kDa protein A class member (cytosolic), protein shock // heat 2 (cytosolic), alpha 90kDa 6 member A class (pseudogene)

96 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3147591 chr8 -3344897 chr11 103907725 103953967 + 7.51 93157019 93186225 7.49 3838185 chr192774971 + chr4 54280358 - 54304714 7.52 80762874 81219758 7.51 3964154 chr22 - 45454343 45537349 7.52

30 (continued) 2 // CMG2 // // CMG2 2 // 35 // DBC1 1 3089597 chr8 + 22518038 22534618 7.49 MGC3832 // MGC3832 // // OAZI MGC691 // ODC1L OAZIN // DRIP80 CRSP77 // FLJ10812 // // TRAP80 MED17 DBC- RNPU1Z // RPU1 // RPU1 // // RNPU1Z // U1AP // U170K U1RNP CMG- // ISH // FLJ31074 // MGC111533 JHF MGC45856 // DKFZp434E0211 // DKFZp434E0211 // FLJ21430 // FLJ23239 // LK4 // KIAA1646 // MGC131878 // dA59H18.2 // dA59H18.3 hCERK 40 015878 015878 021174 021934 FLJ11773 004268 3415273 chr12 + 50749317 50757534 7.51 003089 058172 022766 022766 NM_ // NM_ 148174 NM_ // NM_ 199205 NM_ // 001009820 NM_ NM_ // NM_ 182661

45 C12orf44 NM_ CRSP6 NM_ SNRP70

55 Gene NameGene Symbol Gene Accession Synonym chromosome 12 open 44 frame reading cofactor required for Sp1 activation, transcriptional 6, subunit KIAA196777kDa KIAA1967 anthrax toxin receptor 2 receptor toxin anthrax ANTXR2 1 inhibitor antizyme NM_ AZIN1 small nuclear nuclear small 70kDa ribonucleoprotein antigen) (RNP polypeptide ceramide kinase CERK

97 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3229943 chr93470793 - chr12 1384162103070658 138425418 - 7.49 chr7 108370845 108399528 - 7.48 122968075 122985216 7.48 3607232 chr15 +2963407 chr6 869482542679864 86976501 - chr3 7.47 86374062 - 86410282 7.47 63971281 63984700 7.47

30 B // B // (continued) 13KD- 3 // RBP // RBP // 35 // 113M CO- FLJ13451 // // FLJ13451 // PTFalpha SNAP190 // FLJ41739 // MSTP028 ULRO61 CI- // B13 // DKFZp781K1356 // NUFM FLJ12147 UQOR13 // AEN // FLJ12484 // AEN // FLJ12484 // FLJ12562 pp12744 GRY- NSAP1 HNRPQ1 // // RP1-3J17.2 // // pp68 dJ3J17.2 // S10 // KIAA0107 SGA- p44S10 NY-

40 006643 031954 005000 022767 002859 FLJ16691 006372 3474372 014814 chr12 - 119132644 119187926 7.47 NM_ // 001039707 NM_ // 001039708 NM_ // NM_ 003086

45 KCTD10 NM_ NDUFA5 NM_ SYNCRIP NM_ PSMD6C7orf30 NM_ 138446 NM - 2992863 chr7 + 23305462 23317894 7.46 1SG20L1 NM_ SDCCAG3 // SNAPC4

50 like 1

55 Gene NameGene Symbol Gene Accession Synonym ATPase, 6 ATPase, potassium channel channel potassium tetramerisation domain 10 containing dehydrogenase NADH alpha 1 (ubiquinone) 13kDa 5, subcomplex, stimulated interferon 20kDa- exonuclease gene paxillingene binding, synaptotagmin cytoplasmic RNA protein interacting (prosome, proteasome PXN subunit, 26S macropain) non- open 7 chromosome NM_ frame reading serologically defined colon // small 3 antigen cancer activating RNA nuclear 4, polypeptide complex, 190kDa

98 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3180263 chr93708422 + chr17 96176674 + 96325754 7.43 7151037 71564782714230 7.42 chr4 + 689573 754428 7.41 3735752 chr17 + 72596335 72767744 7.45 3861617 chr19 - 44018883 44034809 7.45 3212294 chr9 - 85772377 85785355 7.45

30 (continued)

35 // EIF5A1 5A // FLJ14753 // // FLJ14753 MGC117350 EIF- // MGC104255 // uORF MGC99547 A uORF // DKFZp686D20235 // DONG1 // // FLJ36550 // FLJ43813 // MGC129615 // RNF3 MGC40413 RNF3A // DKFZp686C06176 DKFZp686C06176 // PRELID4A // SEC14L FLJ35509 // P/ // FLJ35509 L hnRNP- // OKcl.l4 CSBP // FLJ41122 CSBP // FLJ41122 // HNRNPK // TUNP

40 032558 001970 080927ESDN // CLCP1 2686023 chr3 006315 - 99997526 100124598 7.42 003003 001533 002140 002140 XM- // 001130181 NM_ NM_ // 001039573 NM_ NM_ // 001005335 NM_ NM_ // NM_ NM // 031262 031263

45 EIF5ADCBLD2 NM_ VDAC2 NM_ 003375 NM FLJ23841PCGF3 NM_ 3252577 chr10 + 76639941 76661389 7.41 HIATL1 SEC14L1 HNRPL HNRPK

50 like 1 55 dependent anion anion dependent like 1 (S. 1 (S. like Gene NameGene Symbol Gene Accession Synonym eukaryotic translation translation eukaryotic 5A factor initiation LCCL and CUB discoidin, 2 containing domain voltage- 2 channel finger ring group polycomb 3 hippocampus abundant abundant hippocampus transcript- SEC14- cerevisiae) heterogeneous nuclear nuclear heterogeneous L ribonucleoprotein heterogeneous nuclear nuclear heterogeneous K ribonucleoprotein

99 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3904226 chr20 - 33754569 33793768 7.35 3881443 chr20 + 29774755 29853260 7.37 3429460 chr123308619 + chr103310757 103130628 103354079 - chr10 7.39 119029422 - 119124958 7.39 124740316 124774190 7.38

30 (continued) 1 // 1 //

35 // DIL2 2 // CAPER // CAPER // // CAPERalpha DKFZp781 CC1.3 // FLJ44170 C0423 RNPC2 HCC1 // // C20orf1 // HCA519 HCTP4 // // GRIM- TR // // MGC9145 TRXR1 // // TR1 TXNR // FLJ25412 // PDZK8 FLJ34427 bA129M16.2 // // DKFZp781B0249 // FLJ22973 PEGASUS // // // C20orf2 C20orf1 DIL- GD: // FLS353 40 184237 184237 184244 184234 003330 003330 182742 173791 022466 012112 004551 - 014230 - 3329904 chr11 3771297 + chr17 47557156 - 47562663 7.41 71546467 71580323 7.41 NM_ // NM_ // 184241 NM_ // NM_ // 004902 NM_ NM_ // NM_ // 18272.9 NM_ 182743 NM //

45 RBM39 IKZF5 NM_ TPX2 NM_ NDUFS3 NM_ SRP68 NM_

50 S protein 3, S protein coenzyme Q Q coenzyme

55 Gene NameGene Symbol Gene Accession Synonym RNA binding motif protein 39 PDZ domain containing 8 containing domain PDZ PDZD8 5 finger zinc family IKAROS (Pegasus) NM_ microtubule- TPX2, homolog associated, laevis) (Xenopus NADH dehydrogenase dehydrogenase NADH Fe- (ubiquinone) (NADH- 30kDa reductase) particle recognition signal 68kDa reductasethioredoxin 1 TXNRD1

100 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2701595 chr32652410 - chr3 155475346 155524965 + 7.33 3757108 173240112 chr17 173601176 7.33 - 36933431 36938160 7.32 2809245 chr52505501 + chr2 52320949 52432778 + 7.31 130816288 130828310 7.31

30 (continued) 2 // VLAA2 2 35 DDX36 // KIAA1488 MLEL1 // DKFZp686D14170 // DKFZp762K137 // // FAD104 // FLJ23399 // MGC10002 // PRO4979 YVTM2421 // K1CS // K19 CK19 MGC15366 // GPIa CD49B // BR // VLA- // BXDC4 // BXDC4 MGC19606

40 004781 CEB 020865 2318637 022763 chr1 172373 + 002276 7753916 7764072 002203 7.35 3511031 chr13 006190 - ORC2 40394613 40533811 2594569 7.32 chr2 - 201482783 201536750 7.31 000989 - 033416 3145953 chr8 - 99123079 99127371 7.31 NM_

45 USP53VAMP3 019050 NM DKFZp781E1417 NM_ 2741236 chr4FNDC3B + NM_ 120353195ELF1 120436746 7.35 NM_ ITGA2 NM_ DHX36 NM_ IMP4 NM_ ORC2L // MGC39518

50 2 His) Ala- Glu-

55 (yeast) like associated associated Gene NameGene Symbol Gene Accession Synonym like factor 1 (ets 1 (ets factor like ubiquitin specific peptidase peptidase specific ubiquitin 53 vesicle- membrane protein3 (cellubrevin) DEAH (Asp- domain III type fibronectin 3B containing E74- factor) transcription domain 19keratin 2 (CD49B, alpha integrin, VLA- of subunit 2 alpha receptor) KRT19 NM_ box polypeptide 36 polypeptide box ribosomal protein L30 protein ribosomal nucleolar U3 small IMP4, homolog ribonucleoprotein, RPL30(yeast) origin recognition complex, 2- subunit NM_

101 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2831124 chr5 + 138505686 138695245 7.26 2931569 chr6 + 151602720 151721361 7.27 3970338 chrX3647632 chr163671873 + chr16 + 17303441 17664033 + 9092682 7.29 9121055 83291080 83371023 7.28 7.27 3615579 chr153949097 - chr22 27703228 + 28048334 7.30 45109982 45131896 7.29 3147508 chr8 - 103682306 103767558 7.30

30 (continued)

35 1 DKFZp686K0542 // DKFZp686K0542 DKFZp686K23100 // KL4A0723 // MGC9105 AKAP250 // AKAP250 // DKFZp686M0430 DKFZp68600331 DKFZp781F2016 // // DKFZp781F2016 // DKFZp781L0254 SCML1 // FLJ41272 PRO0149 // KIAA0190 UBPO // MGC2621 DKFZp686M05161 DKFZp686M05161 // MGC133289 // ZO- // MGC99627 // MTU1 // MTO2 // TRMT1 // TRMT TRNT1 EGRA // TIEG // TIEG // EGRA TIEG1 40 018834 018834 005100 005100 002539 - 2540157 chr2 - 10485474 10606340 7.27 198270 014117 005153 003257 003257 018006 000979 - 3867223 chr19 - 53810441 53814585 7.29 005655 NM_ // NM_ 199189 NM_ // NM_ 144497 XM_ // 001134060 NM_ NM_ // NM_ 175610 NM_ // 001032282 NM_

45 C16orf72USP10 NM_ AKAP12 NM_ TRMU NM_ NHS TJP1

50 2-

55 10 factor like KLF10 Gene NameGene Symbol Gene Accession Synonym Horan syndrome syndrome Horan ornithine decarboxylase 1 decarboxylase ornithine ODC1 3matrin NM_ MATR3 chromosome 16 open 72 frame reading peptidase specific ubiquitin 10 (PRKA) anchor A kinase 12 (gravin) protein tRNA 5- methylaminomethyl- thiouridylate methyltransferase L18 protein ribosomal Nance- and cataracts (congenital RPL18 anomalies) dental NM_ tight junction protein 1 (zona 1 (zona protein junction tight 1) occludens Kruppel-

102 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2714672 chr43214749 + chr9 1273702 - 13238913417309 7.25 chr12 94099471 941276883638048 + 7.25 chr15 547845662714025 - 54793956 chr4 7.23 86795015 86811600 + 7.23 483010 523985 7.22 2805176 chr5 + 31568161 31590902 7.26

30 (continued) 10 // 10

35 EMP // HLC- // EMP PIG5 // C9orf34 DKFZp686P12242 // Fly20736 // // Nop132 // bA62C3.3 bA62C3.4 // // HG4-1 EBP1 p38-2G4 //DLTS // // LIECG2 C15orf4 // MGC22762 // FLJ20265 // // GP17 FLJ39925 // LAS21 // MGC131903 // PRO4405 RLGS1930 DKFZp667N066 // // DKFZp667N066 // FLJ11193 // FLJ23805 MGC33010

40 006191 006191 005882 017948 022163 017733 018356 006185 NUMA 3380901 chr11 - 71389909 71469367 7.25 NM_ // NM_ 001933 NM_ // 001017405 NM_

45 MRPL46 NM_ PIGG NM_ PA2G4 // PA2G4 // DLST C5orf22 NM_ NUMA1MAEA NM_

50 oxo- associated associated

55 Gene NameGene Symbol Gene Accession Synonym nucleolar protein 8 protein nucleolar NOL8proliferation- NM_ ribosomal mitochondrial L46 protein glycan phosphatidylinositol class biosynthesis, anchor G 2G4, 38kDa // 38kDa 2G4, S- dihydrolipoamide succinyltransferase (E2 (E2 succinyltransferase of 2- component complex) alutarate chromosome 5 open open 5 chromosome 22 frame reading apparatus mitotic nuclear 1 protein erythroblast macrophage attacher

103 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3850363 chr19 -2903343 10457571 chr6 10475233 7.20 +2458289 chr1 33044392 33057253 7.20 - 223655840 223683230 7.19 3918696 chr21 + 33836804 33872881 7.20

30 (continued) 5 // 5 // 35 MGC13170 3868659 chr19 - 55992774 56012596 7.17 EWS 3941907 chr22 + 27994201 28026501 7.19 INrf2 // KIAA0132 // // KIAA0132 // INrf2 // KLHL19 // MGC10630 // MGC1114 // MGC20887 // MGC4407 ADAM- // MGC9454 // D6S113E DKFZp686NO336 // FLJ31942 // // FSRG1 NAT // // KIAA9001 // RNF3 RING3 DHCR148 // LMN2R // PHA // MGC9041 BASS1 // C21orf50 C21orf50 // BASS1 DBP- // FLJ21099 // // FLJ21099 // FLJ33914 // KIAA1019 SON3 NREBP // 40 199249 199249 005243 005243 002296 002296 032195 032195 012289 197941 005104 003129 - 3114832 chr8 + 126063738 126105522 7.20 NM_ // NM_ 199250 NM_ // NM_ 013986 NM_ // NM_ 194442 NM_ // NM_ 138927 NM_ // NM_ // 203500 NM_

45 C19orf48 EWSR1 KEAP1 // KEAP1 // ADAMTS6

50 associated

55 Gene NameGene Symbol Gene Accession Synonym like ECH- chromosome 19 open 48 frame reading bromodomain containing 2 containing bromodomain BRD2 epoxidasesqualene NM_ receptor B lamin SQLE breakpoint sarcoma Ewing 1 region LBR NM_ protein 1 // ADAM // ADAM 1 protein with metallopeptidase 1 type thrombospondin 6 motif, SON DNA binding protein binding DNA SON SON kelch-

104 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2440523 chr12950561 - chr6 1592756652756497 159282355 - 7.17 chr43335907 33354871 33365259 chr11 -2341565 7.16 chr1 + 654679 658269 65573499 + 65593343 7.14 7.14 70443686 70492014 7.12

30 (continued) MLTF // MLTF

35 MP100 // PSA // MP100 3724698 chr17 + 42955347 43057168 7.11 MLTFI // UEF // // MLTFI // FLJ00267 RP11- // FLJ44128 544M22.6 // // C6orf11 BING4 FP221 // ATP5K MGC12532 // SAP145 // // SF3b1 SF3B145 SF3b150 DKFZp686M13204 // p54 dJ677H15.2 // FCHL // FCHL1 // // HYPUP1

40 006310 005452 001067 // TP2A TOP2 007100 3756193 chr17 006842 - 35717597 35847034 7.15 007122 007122 181720 004768 - XM_ // 001128588 NM_ NM_ // NM_ // 207005 NM_ // 001025598 NM_

45 TOP2AATP5I NM_ SF3B2 NM_ NM_ NPEPPS SFRS11 NM USF1// USF1// ARHGAP30

55 Gene NameGene Symbol Gene Accession Synonym rich 11 rich serine- WD repeat domain 46 domain repeat WD (DNA) II topoisomerase WDR46 170kDa alpha H+ synthase, ATP mitochondrial transporting, NM_ E subunit complex, F0 2, subunit 3b, factor splicing 145kDa arginine/ factor, splicing puromycin aminopeptidase sensitive upstream transcription transcription upstream GTPase Rho 1 // factor 30 protein activating

105 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2371255 chr13768015 + chr17 181708036 181834004 - 7.09 2704267 62485987 chr3 62672547 7.08 - 169208832 169296426 7.07 2448073 chr1 - 183532162 183553081 7.10

30 7 (continued) BP //

35 1 // NS1- GGTB // - // GGTB 2342624 chr1 + 76024474 76033333 7.07 DRHC // HUMORF5 // K1AA0054 // MGC163454 GIMPC GPP130// // P138 C1orf16 // EST1C // EST1C // C1orf16 // FLJ23717 // KIAA0250 // SMG- SGA56M DKFZp688K06216 DKFZp688K06216 // FLARA3 // // FLJ10069 // FLJ10411 // FLJ10962 // FLJ35593 // FLJ36593 // HSPC068 // ND1 // KIAA0850 NS- 40 004582 004582 014837 014837 201568 014877 000104 // GLC3A CP1B 2548699 014498 chr2 - 38138730 38196009 7.08 006469 006469 NM_ // NM_ 002440 NM_ // NM_ // 173156 NM_ // NM_ 201569 NM_ // NM_ 016389

45 CYP1B1SPRY2 NM_ 005842 NM // MGC23039 // RABGGTB MSH4 3519309 chr13 - 79683810 79813918 7.07 SMG7 IVNS1ABP

55 Gene NameGene Symbol Gene Accession Synonym 7 homolog, nonsense nonsense homolog, 7 helicase with zinc finger zinc with helicase HELZ 1, family P450, cytochrome 1 B, polypeptide subfamily 2 homolog sprouty (Drosophila) NM_ 4 phosphoprotein golgi Rab GOLPH4 geranylgeranyltransferase, mutS // subunit beta (E. coli) 4 homolog NM_ Smg- decay mRNA mediated (C. elegans) factor influenza virus NS1A NS1A virus influenza protein binding

106 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2844410 chr52686727 chr3 + 179092457 - 179151795 7.03 102780272 102878819 7.02 3177563 chr92847292 chr53092276 + chr8 - 877336202797393 87828205 + 6510364 7.06 chr4 6686394 300595423283991 30115386 7.06 - 7.06 chr102976113 187745970 chr6 1878850484016572 - 7.05 chrX - 32337798 32385342 - 137560317 7.04 137582279 102817114 7.04 102844278 7.03

30 1 (continued)

35 KIAA0200 // Mam- KIAA0200 Mam1 // // FLJ13426 // MGC133303 ZNF- U69274 FLJ21613 // // FLJ21613 // FLJ22643 bA379P1.1 // // SAKI FLJ20303 TRM4 Vps55 // HSPC112 my047 // // // FAT1 CDHF7 hFat1 // ME5 // KNS KINH // UKHC KNS1 FLJ45734 // CD119 IFNGR // // KIAA0026 MORFL2// MRGX

40 014757 014415 024635 017755 015344 015895 RP3- // Gem 005245 014947 2898597 - 017426 chr6 MGC13407 004521 000416 + 2773997 012286 chr4 2408855 24857262 24894306 chr1 - 7.06 - 77254731 77288679 42414807 7.04 42574125 7.05 016201 LCCP 2696309 chr3 - 135527277 135576097 7.06 XM_ // 001126853 NM_

45 ZBTB11 NM_ NSUN2LEPROTL1 NM_ NM_ GMNNFAT NM_ NM_ IFNGR1 NM_ MAK10 NM_ MAML1 50 like 1 like like 1 55 Gene NameGene Symbol Gene Accession Synonym zinc finger and BTB domain BTB domain and finger zinc 11 containing NOL1/NOP2/Sun domain domain NOL1/NOP2/Sun 2 member family, overlapping receptor leptin transcript- replication DNA geminin, inhibitor suppressor tumor FAT (Drosophila) 1 homolog J3 box forkhead 54kDanucleoporin 5B member family kinesin FOXJ3 KIF5B NUP54 receptor gamma interferon 1 NM_ 2 like 4 factor mortality NM_ NM_ mastermind- MORF4L2 NM_ (Drosophila) acid N- acetyltransferase acetyltransferase N- acid (S. cerevisiae) subunit, angiomotin like 2 like angiomotin amino- homolog, MAK10 AMOTL2 NM_

107 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3228007 chr93453177 - chr12 134126584 134220359 - 7.00 47333281 47362268 7.00 2756673 chr4 - 833110 916149 7.00 2744597 chr4 + 140442091 140560627 7.00 3316447 chr11 + 912387 1002226 7.01

30 S2 3193900 chr9 + 137531661 137536331 7.02 (continued)

35 MRP- // 91 PAP // PIP3AP PAP // 2852274 chr5 - 32262872 32348897 7.00 - AOA2 // // ALS4 // DKFZp781B151 // FLJ12840 // FLJ43459 // KIAA0625 2745547 // SCAR1 bA479K20.2 chr4 // FLJ12670 FLJ20436 + 144476834 144615158 7.00 FLJ40395 // // FLJ40395 MGC99654 3- Ga19 // NATH // // Ga19 TBDN100 ADTAB // CLAPA2 // CLAPA2 ADTAB HYPJ HIP9 // //

40 002039 002039 015046 017822 005255 021228 SRA1 057175 007118 tgat 3838757 chr19 + 2802398 chr5 54837204 54853671 7.01 + 14196590 14585215 7.00 012305 016034 CGI- NM_ // NM_ 207123 NM 001040446 XM_ // 001127411 NM_

45 A1 NM_ C12orf41 NM_ GAB1 NARG1TRIO NM_ MTMR12 NM_ SR- AP2A2 NM_ MRPS2 NM_

50 mRNA rich pre- rich

55 protein related Gene NameGene Symbol Gene Accession Synonym associated binding A1 senataxinchromosome 12 open 41 frame reading SETX NM_ GRB2- 1 protein cyclin G associated kinase associated G cyclin GAK splicing factor NMDA NMDA factor splicing 1 regulated receptor domain functional triple (PTPRF myotubularin interacting) 12 protein related SR- alpha 2 subunit serine serine subunit 2 alpha arginine- complex 2. mitochondrial ribosomal ribosomal mitochondrial S2 protein adaptor-

108 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3815165 chr193837796 + chr192940551 747768 chr6 + 763505 53640874 - 6.96 53652090 6.95 7213542 7258526 6.94 2568687 chr2 - 105335877 105501005 6.96 3400034 chr12 + 278104 891189 6.98

30 (continued) T //

35 PTB- 1 // PTB2 // PTB3 // PTB3 // PTB2 pPTB // PTB4 // KIAA1942 GRWD WDR28 RRB1 // // DKFZp781N23103 TRAPA // HNRNPI // HNRPI // // MGC10830 PTB // // MGC8461 PTB- AAG11 // DRAL // DRAL // AAG11 SLIM3 - 2678090 chr3 - 57532172 57558635 6.96 KDP // KIAA0344 // // // KIAA0344 KDP // PHA2C PRKWNK1 40 002819 002819 031991 001450 031485 003144 001660 018979 003828 - 000245 RCCP2 HGFR // 3020343 chr7 3994846 chrX + + 116099694 116230307 149612503 6.97 149684226 6.97 NM_ // NM_ // 031990 NM_ // NM_ 175847 NM_ // 001039492 NM_ // NM_ NM // 201555 201557 XM_ // 001132763 NM_

45 GRWD1SSR1 NM_ NM_ PTBP1 FHL2 WNK1MTMR1 NM_ NM_ MET NM_

50 rich WD repeat WD repeat rich oncogene oncogene 55 Gene NameGene Symbol Gene Accession Synonym ribosylation factor 4factor ribosylation ARF4 glutamate- 1 containing receptor, sequence signal (translocon- alpha alpha) protein associated polypyrimidine tract binding binding tract polypyrimidine 1 protein four and a half LIM domains domains LIM a half and four 2 WNKlysine deficient 1 kinase protein myotubularin related 1 protein met proto- ADP- (hepatocyte growth factor factor growth (hepatocyte receptor)

109 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2367793 chr1 + 171950703 172028914 6.90 2491935 chr2 + 86186849 86222791 6.91 3848689 chr19 -2908474 chr6 79294632647647 7999655 + chr3 6.93 44319983 + 44330383 6.93 151585441 151660841 6.91 2410330 chr13878220 chr20 - + 45865575 45926352 17896912 6.94 17919759 6.94

30 (continued) BETA //

35 FLJ10931 3899346 chr20 - 17855335 17897603 6.89 KHLHX // KLEIP // // KLEIP KHLHX RP3- // KLHLX 383J4.3 DKFZp666K071 // // DKFZp666K071 // FLJ20758 // D12S1889 NKHC // // MY050 SPG10 ELAV1 // HUR // // ELAV1 // MelG // Hua DKFZp686H05241 TIM44 // // D6S182 // FLJ26984 HSP90- HSPC2 // HSP90B HSPCB // // TlLZ4a KIAA0669 // TILZ4c TILZ4b // RP11-767N6.1 // SP192 // FLJ14597 bA504H3.4 40 014426 014426 017952 017952 014458 001419 001419 007355 014779 021639 052865 NM_ // NM_ 152227 NM_ // NM_ 004984 NM_ // NM_ 006351

45 HSP90AB1 NM_ TSC22D2 NM_ PTCD3 // KIF5A GPBP1L1 NM_ C20orf72 NM_ // ELAVL1 TIMM44

55 1 like Gene NameGene Symbol Gene Accession Synonym like 20 (Drosophila) KLHL20 NM_ rich promoter binding binding promoter rich sorting nexin 5 nexin sorting SNX5 kelch- heat shock protein 90kDa 90kDa protein shock heat B class (cytosolic), alpha member 1 family, domain TSC22 member 2 repeat Pentatricopeptide family kinesin 3 // domain 5A member GC- 1- protein chromosome 20 open 72 frame reading lethal, (embryonic ELAV vision, abnormal (Hu 1 Drosophila)-like of // translocase R) antigen mitochondrial inner membrane 44 homolog (yeast)

110 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3759704 chr173371928 - chur112401275 - 40696283 chr1 40750550 47142451 6.85 47155114 - 6.84 23486545 23543926 6.84 3153428 chr8 - 131133540 131525100 6.85 3343452 chr11 + 86189210 86341580 6.87

30 (continued)

35 FTDCR1B // HS // // FTDCR1B // NIK HSNIK // FLJ14576 FLJ26000 // IRZ // Nbla 10535 // Zfp289 // FLJ25714 hnRNP- HNRNPR // R DKFZp781D1727 3609138 // // ASAP1 AMAP1 PAG2 // KIAA1249 chr15ZG14P PAP // // + 91227096 91387351 6.86 PMEPA1 // PMEPA1 STAG1 3911217 chr20 - 55656877 55781123 6.87 MGC5107 // SIG13 // SIG13 MGC5107 SPUVE // ZSIG13 //

40 003954 032389 005826 020198 MSTP041 // GK001 3766334 chr17 - 59176353 59204726 6.84 001271 018482 020182 020182 199170 014487 // NOA36 HSA6591 2745220 chr4 + 142336669 142381405 6.87 007173 NM_ // 001042572 NM_ NM_ // NM_ // 199169 NM_ // NM_ 199171

45 ZNF289 NM_ HNRPRCCDC47 NM_ NM_ MAP3K14 NM_ DDEF1 NM_ CHD2 TMEPAI

55 protein activated Gene NameGene Symbol Gene Accession Synonym coil domain zinc finger protein 289, ID1 ID1 289, protein finger zinc regulated nuclear heterogeneous R ribonucleoprotein coiled- 47 containing kinase kinase kinase 14 kinase kinase kinase development and enhancing differentiation 1 factor mitogen- zinc finger protein 330 protein finger zinc helicase chromodomain ZNF330 2 protein binding DNA NM_ KIAA0179 23 serine, protease, PRSS23transmembrane, prostate KIAA0179 RNA induced androgen NM_ 015056 NM - 3923218 chr21 + 43903644 43940364 6.87

111 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2798586 chr5 +2403111 chr1 324634 491368 - 6.81 27603331 27689256 6.81 3656904 chr16 + 31093395 31111003 6.82 3372253 chr11 -3708798 47444068 chr172487549 47543613 6.83 chr2 +3090922 chr8 7405827 + 7416006 + 69995330 6.82 70023575 26156860 6.82 26286261 6.82

30 (continued) CHOP

35 // 2 CHOP // FUS- // CHOP FUS1 // // CHOP TLS/ // TLS ALG- // MGC111017 // MGC119050 PEF1B // MGC9123 AHH // AHHR // // WAVE2 // SCAR2 dJ393P12.2 BRUNOL2 // CUG- BRUNOL2 // CUGBP BP hNab50 // NAB50 // DKFZP586K0919 // DKFZp762A152 SSP3 // SMT3IP1 // MAD 1 // MAD MGC104659 // // FLJ26613 B55A // MGC52248 PR55A // PR52A 40 013232 013232 006560 004960 006392 NOP56 006990 3873874 chr20 + 2580791 2587030 6.81 007359MLN51 // BTZ 015670 3720739 002357 chr17 002717 + 35518075 35586901 6.82 NM_ // NM_ 020731 NM_ // 001025596 NM_ // NM_ 198700 NM_ // 001010850 NM_

45 NOL5AWASF2 NM_ NM_ PDCD6 // AHRR CASC3SENP3 NM_ NM_ PPP2R2A NM_ FUS CUGBP1

50 16) (12;

55 Gene NameGene Symbol Gene Accession Synonym hydrocarbon receptor receptor hydrocarbon nucleolar protein 5A (56kDa 5A (56kDa protein nucleolar repeat) KKE/D with family, protein WAS member 2 programmed cell death 6 // aryl- repressor cancer susceptibility susceptibility cancer 3 candidate SUMO1/sentrin/SMT3 3 peptidase specific 1 protein dimerization MAX MXD12 phosphatase protein regulatory 2A), (formerly isoform B, alpha subunit NM_ t in (involved fusion in malignant liposarcoma) CUG triplet repeat, RNA repeat, triplet CUG 1 protein binding

112 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3787031 chr18 + 42008011 42123527 6.78 3229529 chr9 - 137840157 137938826 6.81

30 (continued)

35 ARKL1 // // ARKL1 // MGC12909 MGC87799 DKFZP434F195 // // DKFZP434F195 // DKFZp434G2311 // FLJ31228 // MGC163452 // PRO2405 bA100C15.1

40 145055 003590 002451 c86fus // MSAP 014820 3164914 FLJ90470 chr9 2601544 032795 FLJ14494 2686371 chr2 + 152594 chr3 FLJ33903 21792645 - 3396883 22022975 - chr11 6.77 3589141 225025520 225158348 chr15 101565001 - 6.78 101614635 6.76 + 125577202 125586743 6.76 36331548 36468943 6.76 015447 NM_ // 001008239 NM_

45 MTAPTOMM70A NM_ NM_ RPUSD4 NM_ SPRED1 NM_ CAMSAP1 NM_ C18orf25

55 protein associated related, EVH1 related, Gene NameGene Symbol Gene Accession Synonym domain containing 4 containing domain EHD4 139265 NM PAST4 3620276 chr15 - 39977674 40052063 6.75 cullin 3cullin methylthioadenosine phosphorylase outer of translocase mitochondrial membrane A (S. homolog 70 cerevisiae) CUL3RNA pseudouridylate domain synthase 4 containing NM_ sprouty- 1 containing domain EH- calmodulin regulated regulated calmodulin spectrin- 1 chromosome 18 open 25 frame reading

113 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3841949 chr193882681 + chr202356115 60273799 + chr1 60291530 6.74 31862780 + 31905829 6.74 144149846 144164251 6.72 4002148 chrX2808612 - chr5 20052567 + 20069880 6.71 44844784 45054668 6.71 3371986 chr11 - 47169280 47858048 6.74

30 (continued) 4C // 4C S30 // PAP // // PAP S30

35 // eIF- 1A EIF1A // EIF4C // EIF4C // EIF1A eIF- DRC3 // EPS8R1 // // // EPS8R1 DRC3 // FLJ20258 // MGC23164 // MGC4642 PP10566 // C20orf178 SNF7-2 // CHMP4A // Shax1 // // EST01027 // THIF // HHCPA78 VDUP1 DKFZp566B2024 // DKFZp566B2024 MRP- PDCD9 MGC75406 // p55 // MGC75406 3768103 chr17 // MGC150678 MGC150679 - 62764497 62804392 6.75

40 001412 001412 017729 017729 139204 176812 006472 016640 015231 XM_ // 001134077 NM_ // - NM_ // NM_ // 133180 NM_ XM_ // 001134070 XM_ // 001134072 XM_ // 001134073 002816 NM

45 CHMP4B NM_ TXNIP NM_ // EIF1AX EIF1AP1 MRPS30 NM_ PSMD12

50 linked linked

55 Gene NameGene Symbol Gene Accession Synonym like 1 like EPS8L1 ATPase, 12 ATPase, chromatin modifying protein protein modifying chromatin 4B interacting thioredoxin protein translation eukaryotic 1A, X- factor initiation // eukaryotic translation initiation factor ribosomal 1A mitochondrial S30 protein nucleoporin 160kDanucleoporin NUP160EPS8- NM_ proteasome (prosome, (prosome, proteasome subunit, 26S macropain) non-

114 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3377044 chr11 - 64287827 64302817 6.69 3721579 chr172348060 + chr1 37422156 37431177 + 6.70 96959805 97144643 6.70 3185643 chr9 + 115246842 115399812 6.71 3281621 chr10 - 24912552 25052583 6.71

30 (continued)

35 D11S636 // ZFM1 // ZFM1 // D11S636 ZNF162 DKFZP434N1526 // DKFZP434N1526 // KBRAS2 // MGC74742 // MIBP FLJ34897 // // PTBLP PTB // nPTB // brPTB // nPTB6 // nPTB5 nPTB8 // nPTB7 C2PA // FLJ20370 // FLJ20370 // C2PA // FLJ31516 PDZ- // FLJ90496 // RGP3 RGS3 ARHGAP10 // ARHGAP10 // L0424 DKFZp761 FLJ33323 40 004630 004630 201997 144489 144489 017595 021190 017790 017790 130795 144488 020824 NM_ // NM_ // 201995 NM_ // NM_ 201998 NM_ NM_ // 001001349 NM_ NM_ // NM_ // 021106 NM_ // NM_ // 134427 NM_ //

45 PTBP2 NM_ NKIRAS2 ARHGAP21 NM_ RGS3

50 protein

55 Gene NameGene Symbol Gene Accession Synonym like 2 like polypyrimidine tract binding binding tract polypyrimidine 2 protein 1factor splicing SF1 NFKB inhibitor interacting interacting inhibitor NFKB Ras- Rho GTPase activating 21 protein of G- regulator 3 signalling

115 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2966253 chr6 - 99952648 99980235 6.68 3699044 chr16 - 73212799 73258283 6.68 2806799 chr5 + 36894163 37115932 6.68

30 (continued) B // BCON3 // // BCON3 B // 35 DKFZp564B0769 // DKFZp564B0769 // FLJ14752 // FLJ14853 // FLJ14992 // FLJ90147 // HSPC306 // MGC104269 // 98I9.2 RP11- // SRrp130 // bA98I9.2 MGC14793 FLJ10520 // // FLJ10520 RNF201 CDLS // CDLS // DKFZp434L1319 // FLJ11203 // FLJ12597 // FLJ13354 // FLJ13648 // // IDN3 FLJ44854 IDN3- // FLJ27109 // MADM FLJ35541 // MUDPNP // NRBP 40 032870 032870 004323 - 3203482 chr9 - 33237838 33255392 6.68 015384 015384 013392 931094 931094 931124 944255 944273 NM_ XM_ // // 371838 XM_ XM_ // // 931115 XM_ XM_ // // 939661 XM_ XM_ // // 944271 XM_ // NM_ 001080481 NM_ // NM_ // 133433 NM_

45 BAG1 NM_ // C6orf111 USP45 RFWD3 018124 NM NIPBL // NRBP1

55 B homolog B homolog Gene NameGene Symbol Gene Accession Synonym associated associated BCL2- athanogene open 6 chromosome // 111 frame reading peptidase specific ubiquitin 45 ring finger and repeat WD repeat WD and ring finger 3 domain Nipped- nuclear // (Drosophila) 1 protein binding receptor

116 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3368707 chr11 - 336763972395177 33714806 6.65 chr13766893 chr17 -3421630 - 7987071 chr12 8194824 59924843 59935796 6.62 + 6.62 68265508 68281612 6.62 3088405 chr8 + 19666766 19753848 6.67

30 1- 6 // (continued) beta beta 33 // MIG- // 33 35 16.3A5 // EJ16 // EJ16 // 16.3A5 // // EL32 EJ30 // // MGC2354 G344 // // MIN1 MIC11 // // MIN3 MIN2 // MSK21 p18- // PROTECTIN GENE- MIG6 // RALT DKFZp686J01190 // HLR1 G17P1 // // p68 HUMP68 // CCT- 99D8.1 CCTB // // // MGC142074 // MGC142076 // TCP- PRO1633 beta C8orf35 // C8orf35 //INT10 FLJ10569

40 000611 000611 203330 007346 017896 TWA1 018948 004396 3892941 3893072 chr20 chr20 006431 + + 60906461 61039681 60915796 61050570 6.65 6.63 018142 020801 TLIMP // KIAA1376 2866704 chr5 - 90700311 90782084 6.67 NM_ // NM_ // 203329 NM_ // NM_ 203331

45 OGFRC20orf11 NM_ ERRFI1 NM_ NM_ CCT2 NM_ DDX5 NM_ INTS10ARRDC3 NM_ NM_ CD59

50 Asp) Asp) Ala- Glu-

55 Gene NameGene Symbol Gene Accession Synonym opioid growth factor factor growth opioid receptor chromosome 20 open 11 frame reading feedback ERBB receptor 1 inhibitor DEAD (Asp- containing chaperonin 2 (beta) subunit TCP1, box polypeptide 5 polypeptide box dynactin 5 (p25) 5 dynactin subunit complex integrator 10 containing domain arrestin DCTN53 _032486 NM molecule, CD59 p25 // MGC3248 regulatory complement protein 3653042 chr16 + 23560236 23588668 6.67

117 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2819044 chr5 + 86599391 86724647 6.60 3527514 chr14 +3488094 20007398 chr13 20015985 6.61 + 44592617 44756234 6.60

30 (continued)

35 CMAVM // AVM CM- // DKFZp434N071 // PKWS // GAP // RASA // RASGAP // p120GAP SSA2HCKID 2372924 chr1 // MGC117396 // MGC125915 3774823 PNP // MGC125916 + // PRO1837 // chr17PUNP 191281274HMG20 191327514 - 6.62 // RAP30 // BTF4 // TFIIF TF2F2 77789955 3476741 77824878 chr12 6.62 - 123962213 123965631 6.61 40 002890 002890 001893 001893 032334 MGC14595 013375 hABT1 3112543 chr8 2899519 + chr6 117847923 + 117930859 6.60 26661709 26708945 6.59 004600 000270 004128 NM_ // NM_ 022650 XM_ // 001132734 NM_ // NM_ 139062 XM_ // 001132949 021009 NM NM_ // 001042369 NM_ // 001042370 NM_

45 C8orf53ABT1 NM_ NM_ GTF2F2 NM_ RASA1 TROVE2

55 Gene NameGene Symbol Gene Accession Synonym chromosome 8 open open 8 chromosome frame reading basal of activator 1 transcription casein kinase 1, delta kinase casein CSNK1D phosphorylasenucleoside NP Cubiquitin NM_ factor transcription general 30kDa 2, polypeptide IIF, activator protein p21 RAS UBC (GTPase activating protein) 1 TROVE domain family, family, domain TROVE member 2

118 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3470037 chr12 - 106650784 1066792353334025 6.56 chr11 + 63362634 63435067 6.55 3697799 chr16 - 70320417 70400594 6.57 3250019 chr103733938 chr17 + + 70330615 70377158 68695573 6.58 68739952 6.58

30 (continued) 1 35 EMK1 // MGC99619 MGC99619 // EMK1 PAR- // MGC45046 // PFM1 // PFM1 MGC45046 RII- PRKAR2 // // BETA ADTG // ADTG CLAPG1 // MGC18255 GU2 GUB // // RH- // MGC3199 II/GuB // DKFZp762L1710 LDLB // KIAA1381 40 004954 012406 012406 152995 // HOZFP FLJ16294 2768273 152758 FLJ31657 chr4 3100909 - chr8 47543715 47612453 + 6.55 64213088 64392289 6.55 001128 032175 FLJ12787 2815455 chr5 + 72897308 72915109 6.57 024045 018714 NM_ // 001039468 NM_ // 001039469 NM_ // NM_ 017490 NM_ // NM_ 002736 NM_ // 001030007 NM_

45 MARK2 NFXL1YTHDF3 NM_ NM_ PRDM4 // PRDM4 PRKAR2B UTP15 NM_ AP1G1 COG1 NM_ DDX50 NM_ 50 Asp) Asp) Ala- like 1 Glu-

55 protein related Gene NameGene Symbol Gene Accession Synonym microtubule affinity- microtubule box binding- regulating kinase 2 kinase regulating nuclear transcription factor, factor, transcription nuclear X- family, YTH domain member 3 MAP/ dependent, regulatory, type type regulatory, dependent, beta II, UTP15, U3 small nucleolar nucleolar small U3 UTP15, homolog ribonuclooprotein, cerevisiae) (S. 4 // containing domain PR cAMP- kinase, protein complex 1, gamma 1 gamma 1, complex subunit DEAD (Asp- of oligomeric component 1 complex golgi adaptor- box polypeptide 50 polypeptide box

119 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3444252 chr12 - 10742960 10775038 6.51 2437871 chr1 - 154245480 154257371 6.52 3872999 chr193382523 - chr113536663 63758732 chr14 - 63762147 6.54 + 75542387 75599441 54588114 6.53 54606655 6.53 3009959 chr7 + 77004361 77123074 6.54 2810458 chr5 + 56504841 56597388 6.55

30 (continued) RS2 // UBC12 // RS2 35 PEST // CSDA1 // DBPA // // DBPA CSDA1 ZONAB DKFZp686F19123 DKFZp686F19123 // // TLAP // HSD25 TRAPB UBC- // - hUbc12 // // HWNT11 // MGC141946 MGC141948 MISS // MGC23138 c14_5346 // CCFDN // FCP1 // CCFDN 3795312PTP- chr18PTPG1 + 75540799 75617601 6.54 DKFZp761C169 // // DKFZp761C169 GPBP // MGC126339 40 003651 003145 003969 003969 004715 004715 004626 144578 002835 022913 XM_ // 001128341 NM_ NM_ NR_ // 002837 NM_ // NM_ 048368

45 RASEF NM 152573 RAB45 // FLJ31614 3211938 chr9 - 84772206 84937805 6.52 SSR2 WNT11C14orf32 NM_ NM_ PTPN12 NM_ // UBE2M UBE2MP1 GPBP1 NM_ CTDP1

50 receptor receptor terminal hand domain domain hand type MMTV MMTV type 55 conjugating Gene NameGene Symbol Gene Accession Synonym rich promoter binding binding promoter rich cold shock domain proteinA CSDA NM_ containing RAS and EF- RAS and associated protein beta) wingless- family, site integration 11 member chromosome 14 open 32 frame reading receptor, sequence signal (translocon- beta protein tyrosine tyrosine protein non- phosphatase, 12 type ubiquitin- (UBC12 E2M enzyme // ubiquitin- yeast) homolog, E2M enzyme conjugating 1 pseudogene GC- 1 protein CTD (carboxy- polymerase RNA domain, II, polypeptide A) 1 subunit phosphatase,

120 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3732885 chr17 + 64019700 64059052 6.49 3877776 chr20 + 16645421 16670916 6.49 2773023 chr4 - 74158547 74343428 6.50 2532793 chr2 + 233825030 233869050 6.50 3553690 chr143110999 + chr8 102921419 103370656 + 6.50 107351659 107834092 6.50 2550790 chr2 - 43961504 44085128 6.51

30 (continued) 23970 // // 23970

35 16 CAR // CNC // CNC1 DKFZp779L0468 // // MGC17251 // PKR1 MGC24807 // // MGC24807 MGC45309 FLJ22206 // GTAR GTAR // FLJ22206 // NY- KIAA0697 // BR- APG16L // ATG16L // ATG16L APG16L // FLJ00045 // // FLJ10035 // FLJ10828 // FLJ22677 WDR30 CTAK1 // KP78 // KP78 // CTAK1 PAR1A // FLJ10125 // FLJ38829 // FLJ41673 // FLJ42450 // FLJ45656 Nbla00307 CLONE- // // LRP130 GP130 LSFC

40 002734 002734 212472 003092 003092 032217 032217 198890 198890 030803 002376 181354 002556 OSBP1 3374698 chr11 - 59098455 59140193 6.51 NM_ // NM_ // 212471 NM_ NM_ // NM_ 198220 NM_ // NM_ 198889 NM_ // NM_ // 017974 NM_ NMJ_ 133259

45 PRKAR1A SNRPB2 MARK3 NM_ ATG16L1 LRPPRC 50 motif

55 rich PPR- rich Gene NameGene Symbol Gene Accession Synonym microtubule affinity- microtubule like 1 (S. cerevisiae) 1 (S. like dependent, regulatory, type type regulatory, dependent, specific (tissue alpha 1, 1) extinguisher protein kinase, cAMP- kinase, protein small nuclear nuclear small ribonucleoprotein B" polypeptide ankyrin repeat domain 17 domain repeat ankyrin ANKRD17 oxidation resistance 1 resistance oxidation OXR1 related autophagy ATG16 NM_ 16- regulating kinase 3 kinase regulating oxysterol binding proteinbinding oxysterol MAP/ OSBP NM_ leucine- containing

121 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3435681 chr123375340 + chr113233547 122030886 chr10 122033406 - 6.48 +2519860 60926704 chr2 60954030 6170982 6.48 6225410 + 6.47 190198920 190244286 6.46 3892918 chr20 + 60898107 60903524 6.49

30 25 // 25 (continued)

35 J8 3347831 chr11 + 108041010 108316858 6.45 MGG814 // SR- MGG814 SRp25 // FLJ39024 MGC9315 // MGC14439 SPF45 // FLJ20752 // NBLA00058 NS3TP1 Eaf7 // FLJ10914 // // FLJ10914 // Eaf7 // 15SP MRG MRGBP

40 016638 032632PAP // MGC5378 015497 3550392 DKFZP564G2022 014949 3620515 chr14 RP11-336K24.1 004398 chr15 HRH- 2437753 002827 + chr1 PTP1B - 96038038 96104627 - 40289650 6.46 3888721 40353024 154149414 6.46 chr20 154174836 6.45 + 48560298 48634700 6.45 024811 032905 014945 HMFN1661 019048 2834863 chr5 + 148497619 148620192 6.47 018270 NM_ // 001002251 NM_ // 001002252 NM_ // NM_ 018694

45 TMEM87A NM_ PTPN1 NM_ DDX10 NM_ FLJ12529 NM_ RBM17ABL1M3 NM_ NM_ ASNSD1 NM_ C20orf20 NM_ ARL6IP4

50 Asp) Asp) like factor Ala- Glu-

55 Gene NameGene Symbol Gene Accession Synonym ribosylation- (A) polymerase alpha (A) polymerase PAPOLA NM_ mRNA cleavage factor factor cleavage mRNA transmembrane protein protein transmembrane 87A KIAA0907DEAD (Asp- protein 10 polypeptide non- phosphatase, tyrosine KIAA0907 NM_ box pre- subunit kDa 59 1, RNA binding motif protein 17 protein LIM binding actin 3 member family, synthetase asparagine 1 containing domain poly chromosome 20 open 20 frame reading ADP- 4 protein 6 interacting

122 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2934801 chr63419147 + chr12 1613327233030285 161458399 + 6.42 chr7 60940328 + 610861663655628 6.41 chr16 148026213 148129128 6.41 + 29708911 29724778 6.40 2530599 chr2 + 228045122 228134167 6.43 2708922 chr33605832 chr15 - + 186844235 187025506 6.45 83092594 83150653 6.44

30 (continued) 1 //

35 // // IMP2 2 FLJ42439 // // FLJ42439 // KIAA0213 // MAPKKK4 // // MEKK4 MTK1 PRO0412 // KIAA0529 // MGC131982 // MGC149838 // MGC74854 UNPH4 // MGC149834 MGC149835 // OBP KID // KNSL4 OBP- // MGC116938 // MGC116938 RAB // MGC116940 RIP // IMP- p62 // VICKZ2 // KIAA0211 // MGC138437 MGC138439 40 005922 005922 006313 003592 032837 FLJ14775 002532 MGC8530 007317 3769969 018683 RNF114 3742652 chr17 chr17 - 3888474 - chr20 68715100 68740203 5204992 + 6.41 5264204 6.41 47986321 48003818 6.39 014630 941338 941338 NM_ // NM_ 006724 XM_ // NM_ 004504 NM_ // 001007225 006548 NM

45 USP15 NM_ FAM104A NM_ KIF22 NM_ MAP3K4 ZNF592 NM_ IGF2BP2

50 like like

55 protein activated Gene NameGene Symbol Gene Accession Synonym 1 Rev binding protein binding Rev 1 HRB ubiquitin specific peptidase peptidase specific ubiquitin 15 1cullin sequence with family 104, similarity Amember kinesin 88kDa nucleoporin 22 member family CUL1 3 313 protein finger zinc ZNF313 NUP88 NM_ NM_ NM_ kinase kinase kinase 4 kinase kinase kinase mitogen- receptortype 1 insulin- binding protein 2 zinc finger 592 protein HIV- growth factor 2 mRNA 2 factor growth

123 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3795680 chr183550328 chr14 - + 201783 95899075 258461 95923378 6.36 6.35 3409211 chr123214668 + chr9 27567649 277399813132333 - 6.39 chr8 94012330 94096287 - 6.38 38965485 38973467 6.38 2688759 chr3 - 113726408 113769332 6.39

30 (continued)

35 KIAA0401 // // P84 HPR1 P84N5 2489071 // HSPC210 MGC4945 chr2 + 74066761 74188804 6.37 L2 // hSGT2 // hSGT2 // L2 hSgt2p // IARS1 FLJ20736 PRO0785 ILRS // // // BLP1 // MGC125813 MGC125814 APG3 // APG3L // // APG3L APG3 DKFZp564M1178// // FLJ22125 // MGC15201 PC3-96 40 003622 003622 002161 031940 005131 016472 007146 // ZNF161 DB1 3764066 chr17 - 53359568 53420600 6.34 005803 - 2948587 chr6 - 30796156 30818490 6.38 022488 371501 371501 XM_ XM_ // 942026 NM_ // NM_ 177444 NM_ // NM_ 013417 NM_ // 001024380 NM_ // 001024381 NM_ // NM_ 078473

45 C14orf129 NM_ VEZF1 NM_ MGC22014 ATG3 NM_ PPFIBP1

55 tRNA synthetase IARS Gene NameGene Symbol Gene Accession Synonym THO complex 1chromosome 14 open 129 frame reading zinc endothelial vascular THOC1 1 finger NM_ flotillin 1flotillin isoleucyl- FLOT1 2 containing domain TM2 TM2D2 NM_ protein hypothetical MGC22014 ATG3 autophagy related 3 3 related autophagy ATG3 (S. cerevisiae) homolog protein, interacting PTPRF beta 1 (liprin protein binding 1)

124 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3372337 chr112703217 - chr3 47550326 - 47557362 6.32 161663997 161766070 6.31 3395416 chr11 -3420713 122429309 122438895 chr12 6.33 + 65946048 65994719 6.32

30 (continued)

35 BKLHD4 // BKLHD4 // FLJ10450 HSPC252 // IPOA3 // MGC12217 QIP1 // MGC26703 SRP3 // HSC54 // HSC70 // HSC70 // // HSC54 HSP71 // // HSC71 // // HSPA10 HSP73 // LAP1 // MGC131511 // MGC29929 // CD16 // NIP71 // FCG3 // CD16b FCGR3 // DKFZp434M1414 // FLJ10114 // FLJ10929 // FLJ38691 // FLJ90441 TIP120 // KIAA0829 TIP120A // 40 016506 016506 002268 032848 FLJ14827 3432641 chr12 + 112107758 112114543 6.31 006597 006597 000570 018448 NM_ // NM_ 018095 NM_ // NM_ // 153201 NM_

45 KPNA4 NM_ C12orf52 NM_ CAND1 NM_ KBTBD4 HSPA8 // HSPA8 // FCGR3B

50 dissociated 1 dissociated

55 Gene NameGene Symbol Gene Accession Synonym associated and and associated karyopherin alpha 4 alpha karyopherin 3) alpha (importin chromosome 12 open 52 frame reading cullin- neddylation- BTB (POZ) and repeat kelch 4 containing domain heat shock 70kDa protein 8 8 protein 70kDa shock heat low lgG, of fragment Fc // receptor IIIb, affinity (CD16b)

125 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2778980 chr4 - 99888790 100070801 6.30 3928866 chr21 - 31965222 32077764 6.30 3351841 chr11 + 118460803 118470689 6.30 3541137 chr14 +2833924 66896518 chr5 66922983 6.30 + 145296335 145441529 6.30 3910785 chr20 - 54377855 54402553 6.30

30 (continued) 2A // 2A D // PBGD // PBGD D // 2alpha // EIF2 // // EIF2 2alpha 35 EIF- 2 // CBP // E1F4E1 // E1F4E1 CBP // // EIF4F // EIF4EL1 MGC111573 DKFZP434E098 // DKFZP434E098 // FLJ23364 SRA4 // KIAA1172 PBG- UPS EIF- EIF2A // FLJ23654 // MGC149788 // MGC149789 // MGC90410 AIK // ARK1 // AURA // ARK1 // AIK AURORA2 // // MGC34538 // BTAK STK6 // // STK15 // // STK7 EIF- 40 000190 000190 020706 003600 003600 198434 198436 003470 TEF1 // HAUSP 152550 3679564 chr16 - 8893458 8964832 6.30 004094 001587 001968 NM_ // NM_ 001024382 NM_ // NM_ // 198433 NM_ // NM_ // 198435 NM_ // NM_ // 198437 NR_

45 SFRS15 NM_ EIF4E M_ USP7SH3RF2 NM_ NM_ HMBS EIF2S1 NM_ AURKA // STK6P

50 associated)

55 Gene NameGene Symbol Gene Accession Synonym rich 15 rich serine- splicing factor, arginine/ factor, splicing eukaryotic translation translation eukaryotic 4E factor initiation ubiquitin specific peptidase peptidase specific ubiquitin virus- 7 (herpes ring containing domain SH3 2 finger hydroxymethylbilane synthase eukaryotic translation translation eukaryotic 1 2, subunit factor initiation 35kDa alpha, aurora kinase A // serine/ kinase aurora threonine kinase 6 kinase threonine pseudogene

126 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3228373 chr9 - 134756560 134809831 6.27 3942062 chr22 + 283294463263790 28424577 chr10 6.29 3934245 + chr212659039 112317039 chr3 112365483 - 6.28 + 44016298 44020687 196867150 6.28 196953662 6.27 3369890 chr11 - 36465173 36488940 6.29 2882897 chr5 - 154247066 154309713 6.30

30 (continued) 3310 // // 3310 35 KIAA0243 // LAM // // LAM // KIAA0243 TSC // MGC86987 ACN // BANF // BANF // ACN // // SCH Merlin BMH // // BAM // HCAP CSPG6 SMC3L1 // EPM1 // CST6 STFB // PME // FLJ14408 KIAA1359 MGC: RNF85 DKFZP586M1824 DKFZP586M1824 MGC142174 // 40 000368 000368 000268 000268 181825 181829 181831 181833 005445 015221 TUBA // KIAA1010 000100 3303165 152673 chr10 - 101624846 101759656 6.28 004620 004620 016465 _ NM // NM_ 001008567 NM_ // NM_ // 016418 NM_ // NM_ // 181828 NM_ // NM_ // 181830 NM_ // NM_ // 181832 NM_ NM_ 145803 NM //

45 SMC3 NM_ MUC20 NM_ NF2 GEMIN5TRAF6 NM_

50 associated associated

55 Gene NameGene Symbol Gene Accession Synonym structural maintenance of maintenance structural chromosomes 3 protein binding dynamin B)(stefin B cystatin DNMBP 20, cell surface mucin associated NM_ CSTBtuberous sclerosis 1 NM_ TSC1 neurofibromin 2 (bilateral (bilateral 2 neurofibromin neuroma) acoustic gem (nuclear organelle) organelle) (nuclear gem 5 protein associated receptor- TNF 6 factor

127 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3078348 chr7 - 148135436 148212647 6.25 3377226 chr11 - 64376790 64404202 6.26 3431483 chr12 + 109203332 109352495 6.26 2515050 chr2 + 171457150 171551619 6.27 2523689 chr2 + 203901161 204005128 6.27

30 (continued) HSD // RDHL // RDHL // // 1 // EZH1 // // // EZH1 1

35 // ABI2B 2 // // AbIBP3 1 // RDH15 ENX- MGC9169 TREB5 // XBP2 // TREB5 3956589 chr22 - 27520140 27526564 6.25 FLJ42622 // // FLJ42622 H- // FLJ44618 // // HPAST1 PAST // PAST1 PAST ATP2B // DAR // DD // DAR // ATP2B //MGC45367// SERCA2 DKFZP434D156 // DKFZP434D156 // FLJ13139 GOLPH6 // GRS2 // GRASP55 3alpha- // p59 // // RETSDR8 ABI- AIP- // SSH3BP2 // argBPIB argBPIA 40 004456 004456 001681 001681 006795 016403 - 3387171 chr11 - 94322815 94346692 6.26 015530 015530 199204 005759 NM_ 152998 NM // NM_ // 001079539 005080 NM NM_ // NM_ 170665 NM_ // NM_ // 005771 NM_ XM_ 001126750// NM_

45 EZH2 HSPC148 NM_ ATP2A2 GORASP2 // DHRS9

50 reductase reductase

55 Gene NameGene Symbol Gene Accession Synonym domain containing 1 containing domain EHD1 NM_ box binding protein 1 protein binding box XBP1 enhancer of zeste homolog homolog zeste of enhancer 2 (Drosophila) X- hypothetical protein protein hypothetical HSPC148 EH- ATPase, Ca++ Ca++ ATPase, cardiac transporting, muscle, slowtwitch 2 golgi reassembly stacking // 55kDa 2, protein dehydrogenase/ 9 member (SDR family) abl interactor 2 interactor abl AB12

128 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2333429 chr12489411 chr2 + + 43888407 43943994 74609783 6.23 74614240 6.23 2527856 chr2 + 219141552 219170027 6.24 2739079 chr43064638 + chr7 110510304 110681811 - 6.24 3416036 100742601 chr12 1007517932725381 6.24 chr4 + 52132173 + 52161417 6.23 41684531 41812215 6.23

30 (continued) E2

35 JHDM3A // JMJD2// KIAA0677 PARK13 // // OMI PRSS25 FLJ21924 3325768 chr11 + 32871321 32971438 6.22 CNOT9 // RCD1 // // RCD1 // CNOT9 // RCD1+ MGC12837 HNRPE2 // // MGC110998 hnRNP- MGC48822 // // MGC48822 SEC24 // DKFZp761N0823 // FLJ13225 FLJ14117 // // GAC63 C4orf1 // ZNT9 HUEL 40 013247 013247 024774 005444 005444 005016 014663 004447 - 3445908 chr12 - 15664367 15833589 6.23 006323 022777 006345 006298// ZKSCAN8 LD5-1 2900299 chr6 + 28217285 28232872 6.23 _ NM_ 145074 NM // NM_ // NM_ 001076786 NM_ // NM_ 032726 NM_ // NM_ 031989 XM_ // 001130118 NM_ // 001042734 NM_

45 EPS8 NM_ RQCD1 // PLCD4 SLC30A9 NM_ JMJD2A NM RAB L5 NM_ SEC24B

50 like 5 like

55 Gene NameGene Symbol Gene Accession Synonym (rC) binding protein 2 protein binding (rC) PCBP2 HtrA serine peptidase 2 peptidase HtrA serine factor growth epidermal HTRA2 substrate pathway receptor 8 1 rich serine and glutamine QSER1 poly RAB, member RAS RAB, member family- oncogene cell for RCD1 required (S. homolog differentiation C, // phospholipase pombe) 4 delta solute carrier family 30 (zinc transporter), member 9 192 protein finger zinc containing domain jumonji 2A ZNF192 NM_ SEC24 related gene family, family, gene related SEC24 B (S. cerevisiae) member

129 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3597338 chr15 + 611057112949210 61151151 chr6 6.21 - 31736995 31742029 6.21 2615360 chr3 + 30492214 30710745 6.21 3647504 chr162763805 chr4 + 8798971 - 8850664 24128159 6.22 24250940 6.22

30 (continued) RII alpha // alpha 2 // 2 kappa 35 TMSA // alpha ANKRD59 // ANKRD59 // // G5 D6S54E GPANK1 // GPATCH10 TPM1- AAT3 // FAA3 // FAA3 // AAT3 // // MFS2 HNPCC6 // // TAAD2 RIIC TGFR- TGFbeta- HTM- TPM1- // CDG1 // CDG1aCDG1 // CDGS // // DDX15 DBP1 // // PRP43 HRH2 // PRPF43 PrPp43p

40 000366 000366 033177 006067NOC4 // C16orf4 016090 FLJ11153 3703164 chr16 3349918 - chr11 84362936 + 84391266 6.21 113776539 113790335 6.20 003242 000303 001358 NM_ // NM_ // 001018004 NM_ // 001018005 NM_ // 00J018006 NM_ // 001018007 NM_ // 001018008 NM_ 001018020 NM_ // 001024847 NM_

45 BAT4 NM_ TGFBR2 DHX15 NM_

50 His) Ala- Glu-

55 Gene NameGene Symbol Gene Accession Synonym B associated associated B HLA- 4 transcript COX4 neighbour 7 protein motif binding RNA RBM7 COX4NB NM_ NM_ tropomyosin 1 (alpha) 1 tropomyosin TPM1 phosphomannomutase 2phosphomannomutase PMM2DEAH (Asp- NM_ transforming growth factor, (70/80kDa) II receptor beta box polypeptide 15 polypeptide box

130 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3649890 chr16 +3388631 15950935 chr11 16144419 6.18 - 101772285 101828945 6.18 3779756 chr18 + 12886655 12981306 6.17 2892738 chr63982462 + chrX 3966500 + 4010215 6.19 77207320 77269191 6.19

30 (continued) X // MRP // // X // MRP 35 ABC29 // ABCC // // ABC29 DKFZp686N04233 DKFZp781G125 // GS- // MRP1 // PORIMIN // KCT3 PORMIN SEC13L // SEH1A SEC13L // Seh1 SEH1B KlAA0536 // PR4H // // PR4H KlAA0536 // // PRP4H PRP4 // PRP4K dJ1013A10.1 // MGC117307 // MGC142128 MIG10 // MGC8947 PGKA //

40 004996 004996 019898 019900 019902 052932 003168SUPT4H // SPT4H 3764384 003913 chr17 - 000291 53777538 53784705 6.19 NM_ // 001013437 031216 NM NM_ // NM_ // 019862 NM_ // NM_ // 019899 NM_ // NM_ // 019901 NM_

45 SUPT4H1 NM_ PRPF4B NM_ ABCC1

50 mRNA 55 Gene NameGene Symbol Gene Accession Synonym like (S. cerevisiae) (S. like SEH1L binding cassette,sub- transmembrane protein 123 protein transmembrane TMEM123SEH1- NM_ suppressor of Ty 4 homolog homolog 4 Ty of suppressor (S.1 cerevisiae) PRP4 pre- processing factor 4 B (yeast) homolog 1 kinase phosphoglycerate PGK1 NM_ ATP- family C (CFTR/MRP), C (CFTR/MRP), family member 1

131 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2436985 chr13327948 - chr11 153201334 + 1532135103965314 6.15 43337004 chr22 43473027 6.13 - 48552694 48636916 6.12 3190659 chr9 + 130485775 130498483 6.12 3375648 chr11 - 61488337 61492603 6.16

30 (continued) 10 2812120 chr5 + 64100099 64417210 6.15

35 IBETA CO- FLJ26504 // SHC // // SHC // FLJ26504 p52SHC // SHCA // // p66SHC p66 DKFZp686D20222 // FLJ10890 // // FLJ13099 FLJ23673 // // BRPF1 BRL // BRPF2 DKFZp686F0325 // // 12PP2A 2PP2A PHAPII // IGAAD // TAF- - // FTH // FTHL6 // // // FTHL6 // FTH - // MGC104426 // PLIF // PIG15 FTHL5 40 003029 003029 018259 018119 // SIN RPC5 014577 3652489 003011 chr16 + 22216140 22253905 6.13 015535 DKFZp564A2416 005869 2522094 NY- chr2 + 200879035 201053805 6.15 002202 002202 002201 002204 NM_ // NM_ 183001 NR_ // NM_ // 002032 NR_ NR_ - // // // 002205 NR_ NR_ // 002203

45 TTC17POLR3E NM_ NM_ BRD1SET NM_ NM_ SHC1 SDCCAG10 NM_ DNAPTP6 NM_ FTHL7 // FTHL7 // FTH1 // FTHL3 // FTHP1 // FTHL12 // FTHL11 FTHL8 50 like 3 // like 12 // 12 like

55 associated) Gene NameGene Symbol Gene Accession Synonym tetratricopeptide repeat repeat tetratricopeptide 17 domain (RNA) III (DNA polymerase E (80kD) directed) bromodomain polypeptide 1 containing (myeloid SET translocation leukemia- SHC (Src homology 2 homology SHC (Src containing) domain 1 protein transforming serologically defined colon 10 antigen cancer transactivated protein 6 protein transactivated ferritin, heavy polypeptide- heavy ferritin, polypeptide heavy ferritin, // ferritin, 1 pseudogene polypeptide- heavy polypeptide- heavy ferritin, DNA polymerase- like 7 // ferritin, heavy heavy ferritin, 7 // like // ferritin, 1 polypeptide polypeptide- heavy heavy // ferritin, 11 like

132 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2911903 chr6 + 64289625 64351448 6.10 2957700 chr63428131 chr12 - + 53438876 53589510 99185070 6.12 992605643454223 6.12 chr12 - 48657002 48705537 6.09 2429277 chr12651782 - chr3 115061068 115102225 + 6.09 171166446 171194653 6.09

30 (continued) GAP 1 // 1 // 4 // ID-

35 ras // NRAS1 // ras - // DKFZp779M0721 PRL- // HH72 PTP // PRL1 // (CAAX1) PTPCAAX1 3159040HsCYK- chr8 - 145985994 145988615 6.11 GCS // GLCL // // GLCL // GCS GLCLC // CVAK104 // FLJ10074 MgcRacGAP // // D1S155E // DKFZp779B0247 // DKFZp779J1455 RP5- // FLJ26882 // // UNR 1000E10.3 N- Dtrp1 // FLJ32803 // // FLJ32803 Dtrp1 SEC62 // HTP1 40 000973 000973 007158 003463 013277 001498 017988 003262 NM_ // NM_ 033301 NM_ // 001007553 NM_ // NM_ 002524

45 PTP4A1 NM_ RACGAP1 NM_ GCLC NM_ CSDE1 // CSDE1 // NRAS

50 binding binding cysteine ligase, ligase, cysteine 55 Gene NameGene Symbol Gene Accession Synonym like 2 (S. cerevisiae) 2 like SCYL2 NM_ ras) oncogene homolog oncogene ras) protein tyrosine tyrosine protein IVA, type phosphatase member 1 Rac GTPase activating 1 protein glutamate- catalytic subunit SCY1- L8 protein ribosomal RPLB domain shock cold RNA- E1, containing // neuroblastoma RAS viral RAS viral // neuroblastoma (v- translocation protein 1protein translocation TLOC1 NM_

133 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3203382 chr9 - 33031772 33072208 6.06 3507710 chr13 - 28981563 29067721 6.07 3712041 chr17 + 16223047 16228977 6.08 2648141 chr3 + 153444327 153670549 6.08

30 1 // 1 // (continued) 1 35 ATRC1 // CAT- ATRC1 HCATI // ERR // REC1L // FLJ10805 // BWD // FLJ11970 // MGC117363 RP11- 54K16.3 // SMU- FLJ25987 // // FLJ25987 // MGC8385 // FLJ25777 MGC40157 CXorf40 // EOLAI // // EOLAI CXorf40 3994451 chrX + 148413672 148439412 6.08 DKFZp686P06174 DKFZp686P06174 // EXP35 EXP // // // EXP42 // EXP40 MBNL // KIAA0428 40 018225 018955 018955 021038 021038 207293 207295 76124 // 76124 003045 NM_ // NM_ 152350 NM- NM_ 001013845 NM_ // NM_ // 207292 NM_ // NM_ // 207294 NM_ // NM_ NM // 207296 207297

45 SMU1 NM_ SLC7A1 M_ UBB // C17orf45 CXorf40A // // CXorf40A CXorf40B MBNL1

50 52 1 suppressor suppressor 1 like like

55 Gene NameGene Symbol Gene Accession Synonym 8 and unc- and 8 member smu- member mec- of elegans) (C. homolog solute carrier family 7 family carrier solute acid amino (cationic transporter, y+ system),1 ubiquitin B // chromosome // chromosome B ubiquitin 45 frame reading open 17 chromosome X open open X chromosome // 40A frame reading open X chromosome 40B frame reading muscleblind- (Drosophila)

134 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3835814 chr19 + 50041409 4 50084314 6.04 3627248 chr152532064 - chr2 58247806 58482354 + 6.06 3832643 232354256 232382342 chr19 6.06 2876046 chr5 + 43830130 - 43913003 6.06 133557588 133589841 6.05

30 (continued) IV

35 C - 2806256 chr5 + 34965441 34994822 6.03 CD112 // HVEB // // CD112 // PVRR2 PRR2 ANX2 // ANX2L4 // // ANX2L4 ANX2 // LIP2 H // CAL1 LPC2D // // LPC2 PAP- // P36 FLJ12612 // // FLJ12612 MGC111077 DKFZp686K23158 FSGS1 // FSGS // // PP2CA // PP2Ac RP-

40 004039 022730 207356 C17.2 RP13-531 005239 2393816 - 004924 chr1 002715 - 002093 3921068 - 3791939 chr21 3812760 6.06 + 39059147 2691014 39118744 chr3 6.06 - 121018519 121297142 6.05 024845 - 3645901 chr16 + 3433714 3476953 6.04 NM // 001012339 194283 NM NM_ // 001042724 002856 NM NM_ // 001002857 NM_ // 001002858 NM_

45 DNAJA5 PVRL2 COPS7B NM_ C1orf174ETS2 NM_ ACTN4 NM_ PPP2CA NM_ NM_ GSK3BFLJ14154 NM_ NM-

50 related related

55 Gene NameGene Symbol Gene Accession Synonym ets erythroblastosis virus virus erythroblastosis ets DnaJ homology subfamily A member 5 poliovirus receptorpoliovirus 2 (herpesvirus entry entry (herpesvirus 2 B) mediator COP9 constitutive constitutive COP9 photomorphogenic homologysubunit 7B (Arabidopsis) open 1 chromosome 174 frame reading v- E26 2 homolog oncogene 4 alpha actinin, (avian) 2 phosphatase protein subunit, 2A), (formerly isoform alpha catalytic glycogen synthase 3 beta kinase protein hypothetical FLJ14154 annexin A2annexin ANXA2

135 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2418000 chr13275132 - chr10 71292434 - 713558203626555 6.03 5844502 chr15 5924081 6.03 - 56651514 56829469 6.00 3483348 chr133374856 chr11 +3596147 chr15 - 28125188 28151050 + 59330154 5.99 59334921 57628756 5.99 57719710 5.98

30 (continued) 111 110 // UMP1 110 35 DKFZp686J1831 // // DKFZp686J1831 DKFZp686N09117 // ZIS FLJ41119 // // ZIS2 // ZIS1 ZNF265 // FLJ16452 // FLJ37352 RABGDIB CD156c // // MADM HsT18717 kuz // // 013orf12 // HSPCB014 PNAS- FLJ20484 // L16mt L16mt // FLJ20484 PNAS- // // C2GnT- C2/4GnT // C2GnT2 // M

40 005455 005455 001494 001827 CKSHS2 001110 3178583 chr9 015932 + 91050736 91121542 6.01 017840 004751 015324 RRP8 3360982 chr11 - 6492639 6582206 5.98 NM_ // NM_ 203350

45 CKS2ADAM10 NM_ NM_ TERF2ELL2 005652 NM TRF2 // TRBF2 POMP 012081 NM 3696571 NM_ chr16 - 2867873 67946973 68001605 chr5 6.00 - 95246561 95323733 5.99 ZRANB2 MRPL16GCNT3 NM_ NM_

50 binding binding acetyl)

55 Gene NameGene Symbol Gene Accession Synonym zinc finger, RAN- finger, zinc GDP dissociationinhibitor 2 GDI2138 protein transmembrane TMEM138CDC28 protein kinase 2 subunit regulatory NM_ 016464 NM metallopeptidase ADAM HSPC196 10 domain binding repeat telomeric 2 factor 3332886 RNA factor, elongation chr11 II, polymerase maturation proteasome protein + 60885939 60900898 6.02 domain containing 2 containing domain mitochondrial ribosomal ribosomal mitochondrial L16 protein (N- glucosaminyl type 3, mucin transferase KIAA0409 KIAA0409 NM_

136 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3373675 chr113168938 - chr93147321 56823694 + 56848992 chr8 5.98 3405587 37475945 chr12 - 375003793994100 5.97 chrX + 103333634 1034936713473083 5.97 + 12929011 chr12 12986488 1468010983405748 5.96 - 146840329 chr12 5.96 2659631 114868953 chr3 115419724 + 5.96 + 13230082 13264499 198079101 5.95 198143960 5.94

30 (continued) 1 // 1 //

35 20 // EMP- 20 FLJ45975 // // FLJ45975 // KfAA1741 TAB182 // FLJ13390 // PAF53 FLJ13970 // RP11- PRAF1 // 405L18.3 // EDD DD5 // HYD // FLJ11310 // KIAA0896 MGC57263 // // RA13 GPCR5A 1 RAIG FRAXA // // FMRP MGC87458 // DKFZp781D0112 // FLJ21627 // KIAA1025 // MED13L // PROSIT240 TRAP240L CL- TMP // FLJ42398 MGC27076

40 033396 022490 015902 003979 002024 015335 001423 152699

45 TNKS18P1 NM_ POLR1E NM_ EDD1GPRC5A NM_ FMR1 NM_ NM_ THRAP2 NM_ EMP1SENP5 NM_ NM_

55 receptor, coupled Gene NameGene Symbol Gene Accession Synonym tankyrase 1 binding protein protein 1 binding tankyrase 182kDa 1, (RNA) I polymerase 53kDa E, polypeptide ligase, protein ubiquitin E3 1 containing, domain HECT protein- G A 5, member group C, family retardation mental X fragile 1 receptor hormone thyroid 2 protein associated protein membrane epithelial 1 SUMO1/sentrin specific 5 peptidase

137 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop - 1493804 1514582 5.93 Human Genome hg18 Genome Human

20 some Chromo Chromo chr1_ran chr1_ran dom

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2465324 chr13744263 - chr17 245069027 - 245162066 5.92 8034636 8054649 5.92 4045780 3326183 chr11 + 34009711 34081946 5.92 3990566 chrX3442322 + chr12 128832975 - 1289120873837001 5.93 chr19 6824231 6831482 + 5.93 52113779 52200169 5.92

30 (continued) 1 // 1 A // P190A // // P190A A 35 KLAA1722 // 1 DKFZp434N093 // // DKFZp434N093 // // MST108 ELYS // MSTP108 TMBS62 AIM- // AIK2 // // ARK2 AIM1 // // IPL1 AurB STK5 // STK12 FUSIP2 // NSSR // // FUSIP2 // SRp38 // SFRS13 // // TASR SRrp40 TASR2 // TASR1 GP1P137 // M11S1 p137GPI // KIAA0266 // NY- // KIAA0266 // 16 CO- // SDCCAG16 dJ537K23.3 GRCCB // TOME- // MGC2577 1 GRF- // MGC10745 // P190- p190RhoGAP 40 006625 006625 004217 005898 005898 006649 031299 021943 TEX27 // FLJ13222 2905664 004491 chr6 + 37895285 38231400 5.93 015446 NM_ // NM_ 054016 XM_ // 001126456 M_ NM_ // NM_ 203364

45 FUSIP1 AHCTF1 UTP14A NM_ CDCA3ZFAND3 NM_ NM_ GRLF1 NM_ GPIAP1

50 type type rich) 1 rich)

55 Gene NameGene Symbol Gene Accession Synonym arginine- anchored membrane membrane anchored aurora kinase B kinase aurora AURKB NM_ FUS interacting protein protein interacting FUS (serine/ AT hook containing AT hook containing 1 factor transcription UTP14, U3 small nucleolar nucleolar small U3 UTP14, homolog ribonuclooprotein, A (yeast) cell division cycle associated 3 AN1- finger, zinc 3 domain receptor glucocorticoid DNA binding factor 1 GPI- 1 protein

138 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2594497 chr23956290 chr22 - - 201425997 201437659 5.88 26577440 26645487 5.87 2368198 chr12655650 + chr3 173235214 173247469 5.90 +3945877 185499199 chr22 185509504 5.89 + 38226061 38244079 5.88 2621827 chr3 + 48930742 48997971 5.91 3551677 chr14 + 99750383 99818868 5.89 3561039 chr14 - 34940473 34944214 5.90

30 (continued) E1 // E1 // 3 // 3 // 107 // // 107 1 beta // // beta 35 TP- CLK // CLK/STY // // // CLK/STY CLK STY PI- // VIB1B B PtdInsTP GIG5 // MGC87971 // MGC87971 GIG5 PNAS- // // RP1-102G20.6 S1P // S100A6BP // P97 MGC14274 // TRAP2 S2 NF- // DELTA // FLJ20232 // HSU79252 dJ1104E15.3 ARI2 // FLJ10938 II II FLJ10938 // ARI2 // TRIAD FLJ33921 1 YIN- UCRBP // YANG- IKBA // MAD- IKBA NFKBI

40 004071 012399 014412 015871 ZT86 002808 003403 2326311 chr1 019008 + 26368813 26371688 5.90 006321 031450 P5326 // Bles03 3378007 chr11 - 65440893 65443107 5.91 020529 NM_ // 001024646 NM_ NM_ // 001007214 NM_

45 PITPNB NM_ PSMD2 NM_ SMCR7L NM_ ARIH2C11orf68 NM_ NM_ NFKBIA NM_

50 like

55 Gene NameGene Symbol Gene Accession Synonym Magenis syndrome syndrome Magenis like kinase 1 kinase like CLK1 cells inhibitor,alpha ATPase, 2 ATPase, phosphatidylinositol phosphatidylinositol beta protein, transfer zinc finger protein 593 protein finger zinc (prosome, proteasome subunit, 265 macropain) ZNF593non- NM_ factor transcription YY1 YY1 NM_ CDC- ariadne homolog 2 2 homolog ariadne (Drosophila) chromosome 11 open 68 frame reading light of kappa factor nuclear enhancer gene polypeptide B- in Smith- region, chromosome 7- candidate calcyclin binding protein binding calcyclin CACYBP

139 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2464499 chr1 - 243078713 243094575 5.85 3666146 chr163089360 + chr83683050 chr16 668559323392871 + 66893223 chr11 -4007009 5.86 22280765 chrX - 22347587 18719381 5.86 18845318 116153652 - 5.86 116163944 5.86 46886563 46902114 5.86 3434823 chr12 + 120322070 120352805 5.87 3853345 chr193773980 chr17 - - 15351869 15390819 77117366 5.87 77130137 5.87

30 2 A (continued)

35 DKFZp686K15246 DKFZp686K15246 // LAT- KlAA0245 // // y+LAT- // LAT3 2 SAF- HNRNPU // U21.1 // KIAA0062 // LZT- // KIAA0062 cig19 // // ZIP14 Hs4 ATX // // 61E3.4 LIP // KIAA0421 // MGC110983 ZPR1 // ESSS // FLJ20494 // MGC111182 // // Np15 NP17.3 FLJ21786 // RFI // // RIFF RIF DKFZp434L0650 // // DKFZp434L0650 NAKAP // // HAP95 NAKAP95 // FLJ22175 FLJ30151 40 004501 004501 003983 015359 015092 019056 014371 025161 025126 025126 NM_ // NM_ 031844 NM_ // 001076785 NM_ NM- // NM_ 194271

45 SLC39A14 NM_ NDUFB11 NM_ HNRPU SMG1 NM_ SLC7A6 AKAP8L NM_ C17orf70 NM_

50 related kinase kinase related

55 like Gene NameGene Symbol Gene Accession Synonym 1 kinase- 3- solute carrier family 39 (zinc 14 member transporter), PI- 259 protein finger zinc dehydrogenase NADH ZNF259 beta 1 (ubiquinone) 17.3kDa 11, subcomplex, nuclear heterogeneous 003904 NM U ribonucleoprotein factor attachment (scaffold A) SMG- solute carrier family 7 family carrier solute acid amino (cationic transporter, y+ system), member 6 A kinase (PRKA) anchor (PRKA) anchor A kinase 8- protein chromosome 17 open 70 frame reading 34 protein finger ring RNF34

140 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2386867 chr13525679 + chr13 234717161 - 234782890 5.84 110322146 110365417 5.83 3844238 chr193852691 + chr19 63740597 - 63753931 5.84 14380562 14404078 5.84 3902489 chr20 -3975869 chrX 29715925 29775453 + 5.85 46581319 46637601 5.85

30 (continued) 1 // 1 X // xS XL/S // BCL2L XL/S // BCL2L

35 PCTA- 8 // xL // bcl- xL PCTA1 // Po66- // PCTA1 CBP DKFZp686B07190 FLJ20093 // Gal- FLJ29029 // KAP1 FLJ29029 // TF1B // RNF96 TIF1B // BAT1L // BAT1 MGC18203 // DDXL // MGC8417 // URH49 - 3502497 chr13 + 112905835 112967356 5.85 BCL- Bcl- BCLX // // // P2092 DKFZp781 bcl- KIAA0215 // // KIAA0215 TBCCD2 40 006499 006499 201544 017664 001191 001191 005762 005804 003589 006527 HBP 006915 2757319 chr4 - 1664276 1684080 5.85 NM_ // NM_ // 201543 NM_ // NM_ 201545 NM_ // NM_ 138578 NM_ // 001008895 NM_

45 LGALS8 DDX39 NM_ SLBPRP2 NM_ NM_ 50 Asp) Asp) binding, binding, Ala- containing 28 containing TRIM28 NM_ Glu-

55 Gene NameGene Symbol Gene Accession Synonym like 1 like BCL2L1 loop (histone) binding binding (histone) loop ankyrin repeat domain 10 domain repeat ankyrin ANKRD10 NM_ DEAD (Asp- galactoside- lectin, 8) (galectin 8 soluble, box polypeptide 39 polypeptide box tripartite motif- tripartite BCL2- stem- protein (X- 2 pigmentosa retinitis recessive) linked 4Acullin CUL4A

141 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3607927 chr15 + 88529156 88573879 5.80 2485433 chr22562605 + chr2 646049693192653 64714437 - chr9 5.82 2956052 86103197 + chr6 86186509 5.81 134895917 - 134923708 5.81 47307230 47385639 5.80 2903703 chr6 + 33494813 33533290 5.82

30 (continued)

35 DR6 // // 018 KIAA1745 // // KIAA1745 // MGC131831 SemC // SEMAC FLJ20533 // FLJ20080 // FLJ23793 3103494 Nbla // MGC33965 10388 chr8 DKFZP586M0122 // FLJ21915 // // RPA1 MGC87965 + RPO1-4 // // FLJ20857 75046321 // TFIIIC63 // TFIIICepsilon 75057572TFiiiC2-63 5.82 BM- MGC31965 MGC23166 // // MGC23166 G1421 DKFZp761 // KIAA1938 // // // RASA5 RASA1 40 020210 020210 017657 152735 152735 017866 015425 012087 014452 NM_ // NM_ 198925 NM_ // 001002243 NM_ // NM_ 203437 NM_ // NM_ 006772 NM_ // 001040613 NM_

45 POLR1A NM_ GTF3C5 NM_ TNFRSF21 NM_ SEMA48 ZBTB9 // ZBTB9 SYNGAP1

55 Gene NameGene Symbol Gene Accession Synonym aftiphilin (RNA) polymerase 194kDa A, polypeptide AFTPH factor transcription general 63kDa 5, polypeptide IIIC, factor necrosis tumor receptor superfamily, 21 member domain, sema domain immunoglobulin (Ig), transmembrane short and (TM) domain cytoplasmic domain, 4B (semaphorin) transmembrane protein 70 protein transmembrane TMEM70 zinc finger and BTB domain BTB domain and finger zinc Ras 9 // synaptic containing 1 protein activating GTPase (rat) homolog

142 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2352758 chr1 + 114273467 114322014 5.77 3666779 chr16 +3610110 chr15 68156498 682960542793137 + 5.80 chr43667281 94448164 chr16 - 946836203471300 5.79 + chr12 170220651 170428725 5.78 69115212 - 69169072 5.78 109455446 109514152 5.77 3607183 chr15 + 86811688 86822612 5.80

30 2 TFII (continued)

35 KIAA0630 // // KIAA0630 // MGC26642 // MGC33446 // Myak MGC33548 Nbak2 // KIAA0827 // NF- // KIAA0827 // NFATL1 // AT5 OREBP // // NFATZ TONEBP COUP- // ARP1 // COUPTFB // // MGC117452 // SVP40 TFCOUP2 // FLJ21602 // POSH KIAA1494 // RNF142 // // RSE1 KIAA0017 // SAP130 SF3b130 STAF130 // DKFZp686M07120 // MGC133072 // PP2C TA- FLJ22512 // // FLJ22512 HCC- FLJ23406 // 40 152696 152696 198268 006599 006599 138714 022839 022839 021005 020870 012426 139283 NM_ // NM_ // 181358 NM_ // NM_ 198269 NM_ // NM_ // 138713 NM_ // NM_ NM // 173214 173215 NM_ // NM_ 176805

45 NR2F2 NM_ SH3RF1 NM_ SF3B3PPTC7 NM_ NM_ HIPK1 NFAT5 MRPS11

55 Gene NameGene Symbol Gene Accession Synonym cells 5, tonicity- cells nuclear receptor subfamily subfamily receptor nuclear 2 member F, group 2, ring containing domain SH3 1 finger 3, subunit 3b, factor splicing 130kDa phosphatase protein PTC7 (S. cerevisiae) homolog interacting homeodomain 1 kinase protein nuclear factor of activated of activated factor nuclear T- responsive mitochondrial ribosomal ribosomal mitochondrial S11 protein

143 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3219621 chr93729172 chr17 -3178611 + 110744011 chr9 110815625 5.76 55052021 55127299 + 5.76 91122988 91146214 5.74 3066818 chr73749767 - chr17 105625846 - 105713266 5.77 21041205 21058509 5.77 2474527 chr2 + 27504171 27518620 5.77

30 (continued) 17 // // 17

35 CstFp50 // 50 3890154 chr20 + 54393411 54413257 5.77 CLLP // alpha- // CLLP CATU CLH- // CHC17 // // Hc CLTCL2 KIAA0034 DKFZp686C09169 SBP2 // CstF- // 1110035014Rik // DKFZP666B131 // MGC117256 PBEF // // NAMPT LOC646309 // PM1 // C17orf35 PMI BCON3 // BCON3 // // FLJ27109 // MADM FLJ35541 // MUDPNP // NRBP

40 005746 005746 003798 004859 001239 p37 // p34 // CAK 024077 2865860 chr5 - 86707385 86782317 5.74 001 001324 003876 013392 NM_ // - NM_ // 001033521 NM_ // 033522 NM_

45 CTNNAL1 NM_ PBEF1 // PBEF1 RP11- 92J19.4 CSTF1 NRBP1 NM_

50 B cell B cell

55 Gene NameGene Symbol Gene Accession Synonym RNA, subunit 1, subunit RNA, cell colony enhancing enhancing colony cell B- ’ pre- clathrin, heavy chain (Hc) chain heavy clathrin, CLTCcyclin H 2 protein binding SECIS NM_ 26 domain repeat WD SECISBP2 NM_ WDR26 CCNH 025160 NM MIP2 // NM_ FLJ21016 2458082 chr1 - 222639474 222691338 5.74 like 1 like transmembrane protein 11 protein transmembrane TMEM11115 protein transmembrane TMEM115 (cadherin- catenin NM_ associated protein), alpha- 007024 NM PL6 2675304 chr3 - 50367198 50372046 5.76 pre- pre- 1 // factor 1 factor enhancing pseudogene 50kDa nuclear receptor binding binding receptor nuclear 1 protein factor, stimulation cleavage 3

144 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2333635 chr1 +2770427 chr4 44208244 44211909 - 5.72 57496489 57539746 5.72 2330253 chr1 + 36327093 36332113 5.73 3204534 chr93261492 - chr10 35089540 + 35093157 5.74 103901962 103913597 5.73

30 2 (continued) T3 // // T3 T2 // // T2

35 DPH2L2 B4Gal- // B4Gal- // T2 beta4Gal- // HATPL // ATP6F VMA16 // MGC3232 // hAtNOS1 ARH3 // FLJ20446 // FLJ20446 // ARH3 dJ665N4.2 HSPC108 // SLP- // HSPC108 XRCC9 // FAG // // KIAA0035 // NOPP130 // NOPP140 // P130 NS5ATP13 001 001 40 001384 003780 004047 032313 013442 013442 017825 018150 FLJ10597 002572 - 2333907 chr1 + 3350749 chr11 44643293 44889968 + 5.72 116520229 116552810 5.72 004741 NM_ // 001039589 NM_ // NM_ // 005417 NM_ // NM_ // 001039457 NM_ NM_ // NM_ 004629

45 C4orf14 NM_ C1 orf164 NM_ PAFAH1B2 NM_ DPH2 // // B4GALT2 ATP6V0B NOLC1 NM_ STOML2 // // STOML2 FANCG

50 body body Gal:

55 activating factor factor activating Gene NameGene Symbol Gene Accession Synonym ribosylhydrolase like 2 like ribosylhydrolase ADPRHL2 NM_ chromosome 4 open open 4 chromosome 14 frame reading betaGlcNAc beta 1,4- beta betaGlcNAc chromosome 1 open open 1 chromosome 164 frame reading platelet- Ib, isoform acetylhydrolase, betasubunit 30kDa (S. homolog DPH2 cerevisiae) // UDP- galactosyltransferase, H+ 2 // ATPase, polypeptide 21 lysosomal transporting, b subunit V0 kDa, nucleolar and coiled- and nucleolar ADP- phosphoprotein 1 phosphoprotein stomatin (EPB72)-like 2 // 2 (EPB72)-like stomatin anemia, Fanconi G group complementation

145 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3033924 chr7 + 158624381 156754823 5.68 3837836 chr19 + 53664134 53690474 5.69 2534252 chr2 + 238025804 238135783 5.70 3715839 chr173493543 chr13 + + 24095168 24102103 72527115 5.71 72549671 5.70 3355145 chr11 +2675088 125730175 chr3 126063667 5.71 - 50300134 50305282 5.71

30 L (continued) like A

35 KIAA0010 // // KIAA0010 KIAA10 ARNO // CTS18 // CTS18 // ARNO // PSCD2L CTS18.1 Sec7p- // SEC7L // Sec7p- // MGC2771 // MGC2771 // MGC59733 SLAC2- CART1 // MLN62 // MLN62 // // CART1 RNF83 CKLF // // BTEB2 IKLF CGS23 // FLJ11867 FLJ11867 // CGS23 // SAT3 NANTA3 // SIAT4C // S1AT4 // IV // ST3Gal // // STZ ST3GallV // IFNRP FLJ40446 // SM15 SKMcl5 // 40 004228 004228 012255 - 018385 FLJ11301 2711818 3879467 chr3 chr20 - + 195842815 21219705 195874226 21322172 5.69 5.69 145751 145751 024101 001730 006278 002468 - 006764 2617563 chr3 + 38155029 38159513 5.71 NM_ // NM_ 017457 NM_ // NM_ 004295 NM_ // 001042467 NM_

45 LSG1 NM_ PSCD2 KLF5 NM_ MYD88 NM_ TRAF4 ST3GAL4 NM_ IFRD2 NM_

50 associated associated coil domains 2 domains coil 2) related sialyltransferase sialyltransferase galactoside

55 5 factor like Gene NameGene Symbol Gene Accession Synonym 2,3- 3’ exoribonuclease 2 exoribonuclease 3’ XRN2 NM_ ’- large subunit GTPase 1 GTPase subunit large (S. cerevisiae) homolog E3C ligase protein ubiquitin UBE3C 014671 NM 5 (cytohesin- pleckstrin homology, Sec7 Sec7 homology, pleckstrin coiled- and Kruppel- (intestinal) melanophilin MLPH ST3 beta- ST3 differentiation myeloid (88) gene response primary interferon- receptor- TNF 4 factor alpha- 2 regulator developmental 4

146 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3095002 chr8 +3181417 chr9 38973642 39082264 + 5.67 99784907 99823167 5.66 2521500 chr2 + 198088565 198125849 5.67 3397877 chr113076340 - chr7 128343040 128567297 - 5.68 139994192 140274640 5.68

30 (continued) 95 //

35 // GRIT // GAP raf 1 // BRAF1 // // BRAF1 1 raf KIAA0021 // MCMP MCMP // KIAA0021 // Mltng MDC9 // PHAPI2 // // APRIL SSP29 2C4D // CGI- // 2C4D // MGC12264 // MOB3 // MOB1 GROES // // CPN10 HSP10 2H9 3249738 chr10 + 69760947 69772949 5.68 GC- // KIAA0712 // MGC1892 // p200RhoGAP p250GAP B- // 126806 MGC // MGC138284 40 025077 FLJ13949 006401 2334319 chr1 + 45577929 45582381 5.67 015387 015387 002157 032714 MGC13251 3554282 chr14 + 104227008 104244902 5.67 012207 012207 032869 FLJ14991 // CML66 005257 3148796 - chr8 - 3781245 110322324 chr18 110415934 5.68 + 18003412 18060817 5.67 014715 004333 NM_ // 001005845 003816 NM NM_ 11 NM_ // 199482 NM_ NM_ // NM_ 021644

45 TOE1ANP32B NM_ NM_ C14orf151 NM_ ADAM9 PREI3 // HSPE1 RICS NM_ BRAFHNRPH3 NM_

50 rich) nuclear nuclear rich) activating activating

55 Gene NameGene Symbol Gene Accession Synonym raf murine sarcoma viral viral sarcoma raf murine target of EGR1, member 1 1 member of EGR1, target (nuclear) (leucine- acidic family, 32 phosphoprotein member B chromosome 14 open 151 frame reading metallopeptidase ADAM gamma) 9 (meltrin domain NudC domainNudC containing 1 NUDCD1 6 protein binding GATA GATA6 3 // protein NM_ preimplantation 1 protein 10kDa shock heat 10) (chaperonin NM_ Rho GTPase- Rho protein v- B1 homolog oncogene nuclear heterogeneous H3 (2H9) ribonucleoprotein

147 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3014764 chr72831932 chr5 + + 988745153017206 98905314 chr7 140006890 5.66 1400222293878934 5.66 + chr20 102771969 + 102797076 5.65 19935711 19962808 5.65 3277468 chr103403140 - chr122520291 11523200 chr2 11725919 + 5.65 6949871 + 6966191 191453802 5.65 191538513 5.65

30 (continued)

35 CPSF30 // NAR // // CPSF30 NEB1 // IK protein CSA2 // RED // MGC59741 MSS1 // MGC3004 // S7 Nbla10058 // // NAT3 dJ1002M8.1 KIAA0019 // // KIAA0019 TRE2NL RNTRE // // Grcc2f // C2F NEP1 DKFZp686015119 GLS1 // FLJ10358 // KIAA0838 // 40 006693 006083 002703 // GPAT ATASE 2770242 002803 chr4 016100 181528 - 56954288 57029053 5.65 006331 014905 374768 374768 938665 NM_ // 001081559 NM_ NM_ // NM_ // 181527 NM_ XM_ XM_ // // 927409 XM_ XM_ // NM // 943800 001080491

45 IKPPAT NM_ PSMC2 NM_ NM_ EMG1 NM_ CPSF4

50 regulator regulator

55 like terminal USP6NL Gene NameGene Symbol Gene Accession Synonym acetyltransferase 5 acetyltransferase NAT5 IK cytokine, down- IK cytokine, HLA II of phosphoribosyl pyrophosphate amidotransferase (prosome, proteasome subunit, 26S macropain) 2 ATPase, N- USP6 N- EMG1 nucleolar protein protein nucleolar EMG1 (S. cerevisiae) homolog glutaminase GLS NM_ cleavage and and cleavage specific polyadenylation 30kDa 4, factor

148 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3501661 chr13 + 110565635 110756075 5.61 2779992 chr4 - 103934623 104009473 5.61

30 (continued) KB3 // PIX // 35 (17) E2 BETA- // COOL1 // DKFZp761K1021 // KIAA0142 // KIAA0412 // P50 // Nbla10314 // P85 // P50BP // P85COOL1 PAK3 // // P85SPR MGC43926 // // MGC43926 // MGC5416 UBCH5C // UBC4/5 KIAA0079 3251848 chr10 + 75174138 75210008 5.62 BLP2 3642358 chr15 - 99977972 100010609 5.62 40 003899 003899 003340 003340 161867 181889 181891 181893 004922 004922 025141 025141 NM_ // NM_ 145735 NM_ // NM_ // 181886 NM_ // NM_ // 181888 NM_ // NM_ // 181890 NM_ // NM_ // 181892 NM_ NM_ // NM_ 198597 NM_ // NM_ 078474

45 ARHGEF7 UBE2D3 SEC24C PLAGL2 002657 NM FLJ23283 3902682 chr20 - 30243975 30259284 5.63

55 conjugating Gene NameGene Symbol Gene Accession Synonym like 2 like Rho guanine nucleotide nucleotide guanine Rho 7 (GEF) factor exchange ubiquitin- 3 (UBC4/5 E2D enzyme yeast) homolog, SEC24 related gene family, family, gene related SEC24 C (S. cerevisiae) member pleiomorphic adenoma adenoma pleiomorphic gene- 3 containing domain TM2 TM2D3

149 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2890148 chr53194896 - chr9 1789701553764399 178993890 + 5.57 chr17 138896205 - 138943484 5.56 53785272 53849935 5.56 3204404 chr9 - 35026106 35062648 5.58 3114618 chr8 + 125556189 125570389 5.59

30 (continued) 45012 // 45012 35 - DKFZp686A15170 2383726 HNRPH // // hnRNPH chr1MGC: + // TRAP3 TRAP DKFZp781H02126 226313262 DKFZp781H0392 // // FLJ20315 // 226353506 // MGC125630 5.58 // RNF124 URCC IBMPFD // // IBMPFD // MGC131997 // MGC148092 TERA // MGC8560 // FAG // p97 // HRCA1 // // RCA1 MGC31961 TRC8 //

40 007126 007126 001658 006698 BC10 005520 032346 3904928 MGC13096 021138 chr20 3829751 - 017763 chr19 35554050 + 35589711 5.57 39587143 39608910 5.57 007218 NM_ // NM_ 004629 NM_ // 001024226 NM_ // 001024227 NM_ // 001024228 NM_

45 BLCAPHNRPH1 NM_ NM_ PDCD2LTRAF2 NM_ NM_ VCP // FANCG 50 associated associated

55 containing protein // protein containing Gene NameGene Symbol Gene Accession Synonym ribosylation factor 1factor ribosylation ARF1 bladder cancer associated associated cancer bladder protein nuclear heterogeneous H1 (H) ribonucleoprotein 2- death cell programmed like receptor- TNF 2 factor 43 protein finger ring RNF43 NM_ ADP- ring finger protein 139 protein finger ring RNF139valosin- anemia, Fanconi G group complementation NM_

150 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2773756 chr4 -3597603 76786807 chr15 76869171 5.54 + 61554385 61673885 5.54 2910680 chr6 + 53695560 53897416 5.54 2586603 chr23717395 chr17 - + 171538552 171796060 27258855 5.55 27352177 5.55

30 (continued)

35 - // MGC119326 // // MGC119326 - // MGC119329 // ROR1 // NR1F1 ROR3ROR2 // // RZRA // MGC129678 // MGC129879 // UBP SIH003 FLJ10775 // // FLJ10775 LANO // FLJ11834 // dJ523E19.1 // // CBP3 // BFZB // MGC104353 MGC141902 KIAA0137 // PKU- // KIAA0137 BETA // // JJAZ1 CHET9 KIAA0160 40 012297 012297 203505 024611 134260 018214 018214 199487 006537 012290 015355 016221 - 2881554 chr5 - 150065753 150135890 5.54 NM_ // NM_ // 203504 NM_ // NM_ // 001018089 NM_ // NM_ // 002943 NM_ // NM_ NM // 134261 134262 NM_ // NM_ // 018244 NM_ // NM_ 199513

45 USP3 NM_ G3BP2 // G3BP2 // NARG2 // RORA SUZ12 NM_ LRRC1 // C20orf44

50 related related

55 like kinase 1kinase like TLK1 NM_ Gene NameGene Symbol Gene Accession Synonym ubiquitin specific peptidase peptidase specific ubiquitin 3 GTPase activating protein binding domain) (SH3 receptor 2 // NMDA protein // RAR- 2 regulated A receptor orphan tousled- 12 zeste of suppressor (Drosophila) homolog (p62)dynactin 4 repeat rich leucine chromosome // 1 containing DCTN4 44 frame reading open 20 NM_

151 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2978876 chr6 -4009238 149811664 chrX 149908884 5.54 - 53417797 53466400 5.53 2532021 chr2 + 232280604 232286493 5.52 3726934 chr172328713 + chr1 465646932344888 46594905 + chr1 5.52 32417884 + 32436467 5.52 85816676 85867516 5.52

30 H1 (continued) 1

35 HDCME13P // // APC1 // DKFZp686G0123 SCAMC- DKFZp686L19178 DKFZp686L19178 // DXS423E // // KIAA0178 // MGC138332 // SMC1 // SB1.8 SMC1 // SMC1L1 // alpha AWD // // NME2 NDPKA // GAAD // // NM23- NM23 // MGC104802 TMSA // - DKFZp451J0118 // // DKFZp451J0118 MGC118870 // IL14 // MGC118871 // // RP4-622L5.4 - // TXLN // GIG1 // CON1 IGFBP10 40 000269 198175 175852 002823 139126 139126 213651 006306 001554 940631 NM_ // 001018136 NM_ // NM_ NM_ XM_ // // 926306 XM_ NM_ XM_ // // 001127718 NM_ 001045477 NM_ // NM_ // 013386 NM_

45 NME2 SMC1A NM_ NME1- // NME1 TXLNA // DCDC2B CYR61 NM_ // PTMA FAM22G PPIL4 // PPIL4 SLC25A24

50 metastatic

55 angiogenic rich, Gene NameGene Symbol Gene Accession Synonym LV // non- LV structural maintenance of maintenance structural chromosomes 1A NM23- cells 1, protein (NM23A) (NM23A) protein 1, cells in expressed taxilin alpha // doublecortin doublecortin // alpha taxilin 2B containing domain cysteine- 61 inducer, (gene alpha prothymosin, with // family 28) sequence similarity sequence peptidylprolyl isomerase isomerase peptidylprolyl solute 4 // (cyclophilin)-like 25 family carrier carrier; (mitochondrial member carrier), phosphate 24

152 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3262433 chr10 +3284596 105716666 chr10 105778975 5.49 - 34413632 35144249 5.49 3427820 chr12 + 97511471 97519906 5.50 3960478 chr222957126 - chr6 37010115 37150916 - 5.51 52236739 52356643 5.50

30 (continued) 48 // cl.

35 P1.h // MCM3 KIAA0204 // // KIAA0204 // MGC133067 // bA16H23.1 STK2 se20-9 // // // Baz ASIP // Bazooka // // PAR3 FLJ21015 // PAR3alpha // PARD3A // SE2-5L16 SE2- // SE2-5LT1 OK/SW- PHC HCKIE // //- MGC10398 HCC5 // MGC1157 P1- // RLFB // 40 213612 213612 005888 001894 001894 014720 019619 018992 FLJ20040 3645204 chr16 + 2640820 2700477 5.50 002388 929784 929784 NM_ // NM_ // 002635 NM_ // NM_ 213611 NM_ // NM_ // 152221 XM_ XM_ // 940170

45 PARD3 NM_ SLK NM_ KCTD5 NM_ MCM3 NM_ SLC25A3 CSNK1E // CSNK1E // KIAA1660

55 Gene NameGene Symbol Gene Accession Synonym 3 partitioning defective glutathione reductaseglutathione GSRpar- elegans) (C. homolog 3 000637 NM MGC78522 3130161 chr8 - 30655000 30705038 5.49 like kinase (yeast) kinase like potassium channel channel potassium tetramerisation 5 STE20- containing domain MCM3 minichromosome minichromosome MCM3 (S. 3 deficient maintenance cerevisiae) 25 family carrier solute carrier, (mitochondrial member carrier), phosphate 3 22, member G casein casein G member 22, // 1, epsilon kinase protein KIAA1660

153 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2402068 chr1 - 25324131 25431599 5.47 2325526 chr13673515 + chr16 24830814 +3325307 24929968 chr11 5.49 87152329 87225870 + 5.49 31487883 31764940 5.48

30 (continued) 1 48 // WDR50 // 48 3726992 chr17 + 46692081 46730289 5.49 35 KD // CBPIN // // DKFZp56402082 // P29 // NTC31 MAD2 // // MGC43220 // MXI // MXD2 // DJ465N24.2.1 RP3-NPD014 // 465N24.4 160- // MGC39488 // SRM160 POP101 FLJ42528 // // FLJ22664 // FLJ34530 FLJ36075 // C11orf19 // FLJ20498 // PAX6NEB PAXNEB // dJ68P15A. 40 015484 015484 005962 020317 000127 // ttv EXT 3150060 chr8 - 118880792 119193382 5.46 005839 005839 144604 014613 // KIAA0887 ETEA 2842570 019040 chr5 017786 + GOLSYN 175807217 175870117 3148871 5.48 chr8 - 110655383 110964912 5.48 016001 CGI- NM_ // NM_ // 207170 NM_ // 001008541 NM_ // NM_ // 130439 NM_ NM_ // NM_ 001010980

45 NHN1 NM_ ELP4FLJ20366 NM_ NM_ // MXI1 SYF2 orf63 // C1 UTP18 NM_ // SRRM1 C1orf130

55 Gene NameGene Symbol Gene Accession Synonym arginine repetitive exostoses (multiple) 1 (multiple) exostoses EXT1 NM_ conserved nuclear protein protein nuclear conserved NHN1 8 containing domain UBX UBXD8 4 protein elongation (S. cerevisiae) homolog NM_ protein hypothetical FLJ20366 SYF2 homolog, RNA (S. factor splicing MAX // cerevisiae) // chromosome 1 interactor 63 frame reading open 1 UTP18. small subunit subunit small UTP18. (SSU) processome homolog component, (yeast) serine/ 1 // chromosome 1 matrix 130 frame reading open

154 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3212143 chr9 - 85464717 85512928 5.44 3449368 chr123340913 - chr11 30753755 + 30799712 5.44 75803897 75941697 5.44 2575134 chr2 - 128317597 128334003 5.45

30 1 (continued) 1 // EEG1 // // EEG1 1 35 // // DIO1 1 DA41 // DSK2 // DSK2 // // DA41 PLIC- // FLJ90054 // // BYE1 XDRP1 // // DATFI C20orf158 // DIDO2 // DIDO3 // DIO- // DKFZp434P1115 // FLJ11265 // KIAA0333 // MGC16140 EEG- // FLJ11391 // FLJ22569 // MGC102894 // MGC134847 MGC134848 FLJ90741 // EMSY GL002 // MGC50828 3336857 chr11 + 66812660 66826524 5.45 HSRBP4 // HSRBP4 // RBP4 // HSRPB4 // FLJ11294 WDC146 40 013438 013438 022105 080796 023925 020193 138421 FLJ41463 3365249 chr11 - 18048076 18084203 5.45 004805 004805 018383 NM_ // NM_ // 053067 NM_ // NM_ // 033081 NM_ // NM_ 080797 NM_ // 001002259 NM_ // NM_ 032156 XM_ // 001129739 207354 NM NM_ // NM_ // 001006622 NM_ // 001006623 NM_

45 UBQLN1 // UBQLN1 // DIDO1 C 11 orf30 11 C NM_ ANKRD13D POLR2D // // POLR2D WDR33

50 like 1 like SAAL1 NM_

55 Gene NameGene Symbol Gene Accession Synonym obliterator 1 obliterator chromosome 11 open 30 frame reading inducer- death 1 // ubiquilin serum amyloid A- 1 containing domain C1q C1QDC1 ankyrin repeat domain 13 13 domain repeat ankyrin D member family, polymerase (RNA) II (DNA (RNA) II polymerase // D polypeptide directed) 33 domain repeat WD

155 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3507798 chr13 - 29200782 29371040 5.42 2815331 chr5 + 72704665 72850839 5.43 3908831 chr203504434 - chr132798777 chr5 47233911 - 47420063 5.44 20251014 + 20375187 608522 5.43 720187 5.43 3474344 chr12 - 119118908 119123401 5.44

30 1 (continued) NAC // 35 ABC27 // ABC50 // ABC27 2901687 chr6 + 30647103 30667268 5.42 DKFZP434K151 // DKFZP434K151 HCG- // FLJ32018 PNSC1 // BETA- // // BTF3b BTF3a NACB KIAA1694 3670772 chr16 + 80030441 80323852 5.42 FLJ39275 // // FLJ39275 // MGC131926 // PP4052 PRO2521 // FLJ13046 KIAA1721 // FLJ10565 // KIAA1519 MGC5307 BLOCK 23 // L10E // // L10E 23 // BLOCK // 11226 MOC1 // P0 // MOC88175 // RPPO PRLPO 40 001090 030629 030629 001207 001802 // Yo CDR62 3684782 chr16 - 22264766 22356527 5.42 02 1 035 1 035 02 018530 022459 018140 053275 017813 017813 015741 // // 015741 007106 NM_ // 001025091 NM_ NM_ // NM_ 198390 NM_ // 001037637 NM_ NM_ // NM_ // 001042471 NM_ XR- XR_ // NM_ // 001002 NM_

45 // like ABCF1 CDR2 NM_ ZNFX1 // ZNFX1 GSDML RPLP0- RPLPO

50 type type

55 3 like UBL3 M_ Gene NameGene Symbol Gene Accession Synonym inducing protein inducing CMIP binding cassette,sub- Maf- ATP- family F (GCN20), member member F (GCN20), family 1 c- degeneration- cerebellar 2. 62kDa protein related ubiquitin- exportin 4exportin 72kDa protein centrosomal CEP723 factor transcription basic XPO4 NM_ BTF3 NM_ like zinc finger, NFX1- finger, zinc gasdermin- 1 // containing similar to ribosomal protein protein, // ribosomal P0 P0 large,

156 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3716481 chr172474651 + chr23372459 25828452 chr11 + 258935943621728 5.40 - 27659393 chr15 27699586 47694235 5.40 - 47745657 5.39 41950261 42274751 5.39 3831260 chr19 + 41397873 41421503 5.40 2529782 chr2 + 224530378 224540666 5.41

30 (continued)

35 GOS28 // // GOS28/P28 // P28 GS28 // KIAA1805 MGC111046 // DKFZp77911064 // FLJ41904 FBP30 KIAA1014 // // FLJ41022 MGC14161 MGC125660 // MGC125660 // OZF MGC125661 // HZF3 // MGC126498 AXIN // MGC52315 AXIN 3675047 // FLJ12701 chr16FLJ13990 - 277442 351633 5.41 40 032434 015308 173831 - 032892 005627 SGK1 3119765 chr8 2975014 chr6 + - 144771273 144849532 5.39 134532088 134680889 5.38 007145 007145 003415 003502 003502 022915 020673 MGC16770 3890870 chr20 + 56318177 56375962 5.42 NM_ // 001007024 NM_ // 001007025 004871 NM NM_ // NM_ // 152943 NM_ NM_ // NM_ 181050

45 SGK NM_ GOSR1 MRPL44 NM_ // ZNF146 ZNF268 RAB22A NM_

55 Gene NameGene Symbol Gene Accession Synonym glucocorticoid glucocorticoid zinc finger protein 512 protein finger zinc ZNF512formin binding protein 4 FNBP4 707 protein finger zinc NM_ 5containing domain FERM ZNF707 FRMD5 NM_ serum/ regulated NM_ NM_ golgi SNAP receptor SNAP receptor golgi complex member 1 mitochondrial ribosomal ribosomal mitochondrial L44 protein // zinc 146 protein finger zinc 268 protein finger RAB22A, member RAS member RAB22A, family oncogene 1axin AXIN1

157 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2700365 chr33686339 - chr16 150567718 - 150578270 5.34 28016804 28130734 5.34 3570049 chr14 - 68916605 68935306 5.35 3809324 chr183438027 chr12 - + 52334063 52469773 129922411 5.37 129928164 5.36 3539070 chr14 + 61225495 61285222 5.38

30 (continued) 1 //

35 // HIF1- 1 alpha L6 //L6 // M3S1 // H- TAAL6 // FLJ22519 // EXP6 // KIAA0370 RANBP20 DROER // DROER FLJ27340 TRP32 // TXL- TxI // TXNL // Gsp1 // ARA24 TC4 MIG13 3851603 chr19 - 12647534 12653680 5.37 HIF- // // MOP1 ALPHA PASD8

40 006033 // // EL EDL 015171 3787855 018348 - chr18 + 45341077 3697563 45481323 chr16 5.34 - 69872813 69881003 5.34 004450 004786 006325 006141LIC2 // DNCLI2 3695199 chr16 - 65312304 65343212 5.36 001530 001530 001930 013407 014220 XM_ // 001130537 NM_ NM_ // NM_ 181054 NM_ // NM_ // 013406 NM_

45 FLJ11171 NM_ TM4SF1 M_ RANDYNC1LI2 NM_ NM_ ERH HIF1A 50 like 1 like TXNL1 NM_

55 1, factor inducible Gene NameGene Symbol Gene Accession Synonym helix transcription transcription helix lipase, endotheliallipase, 6exportin UPG protein hypothetical FLJ11171 NM_ XPO6 NM_ transmembrane 4 L six 1 member family RAN, member RAS family oncogene light 1, cytoplasmic dynein, 2 chain intermediate rudimentary of enhancer (Drosophila) homolog thioredoxin- deoxyhypusine synthasedeoxyhypusine DHPS hypoxia- helix- (basic subunit alpha loop- factor)

158 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3825383 chr19 + 188037573789947 18840030 chr18 5.34 +3254521 53862627 chr10 54232131 5.30 + 82203922 82272901 5.30

30 (continued) 1 3736290 chr17 + 73721882 73733311 5.29

35 // TM4F2 API4 // EPR- // API4 PEBP2B 3665116 chr16 + 65620522 65692457 5.30 FLJ43809 // // FLJ43809 HUPF1 // FLJ46894 // KIAA0221 // // // RENT1 NORF1 pNORF1 // FLJ33870 // RSP5 KIAA0439 // hNedd4-2 // FLJ20590 // KIAA1619 MGC102867 DC- // MGC11352 TM4SF14 40 001755 001755 001168 015277 015277 002911 030927 NM_ // NM_ 022845 NM_ // 001012270 NM_ // 001012271 NM_ NM_ // NM_ 017893

45 BIRC5 UPF1 NM_ CBFB NEDD4L // SEMA4G

50 like // sema sema // like

55 Gene NameGene Symbol Gene Accession Synonym binding factor, beta baculoviral IAP repeat- IAP baculoviral containing 5 (survivin) containing UPF1 regulator of of regulator UPF1 transcripts nonsense (yeast) homolog 6surfeit cell precursor neural expressed, down- developmentally SURF6 006753 NM 14tetraspanin FLJ30322core- subunit 3228621 TSPAN14 chr9 NM_ - 135186667 135193036 5.32 regulated 4- regulated immunoglobulin domain, (Ig), domain transmembrane domain cytoplasmic short and (TM) domain, (semaphorin) 4G

159 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3173880 chr9 + 70925894 71059931 5.27 2936857 chr63839276 + chr19 167970473 168115537 + 5.28 55524771 55578457 5.28 3109687 chr8 + 102573566 1027511103090697 5.29 chr8 + 25362573 25431420 5.28

30 (continued) I // I // 2 // ZO2 2 // 35 LXRB // b // 6 // AF6 // AF6 // 6 // AF- // AFADIN // FLJ34371 RP3-431 P23.3 LXR- NER- NER // UNR // RIP15 // X104 MGC26306 ZO- // BOM // D FNA28 // // D FNA28 BOM // FLJ11172 // FLJ13782 // MGC149294 // MGC149295 TFCP2L3 // FLJ25804 // MGC129906 // MGC129907 Man Repo-

40 004817 004817 005936 007121 024915 007265 HSGT1 // GCR2 032509 3294242 // MAK16L MAK16 3093259 chr10 152562 chr8 - + 74559939 74598411 33462192 5.29 33478316 5.28 NM_ // NM_ 201629 NM_ // 001040000 NM_ // 001040001 NM_

45 NR1H2 NM_ MLLT4 GRHL2 NM_ ECDRBM13 NM_ NM_ CDCA2 NM_

50 like 2 2 like

55 or mixed- lymphoid Gene NameGene Symbol Gene Accession Synonym Drosophila); translocated translocated Drosophila); receptor nuclear to, H, group 1, subfamily member 2 (zona 2 protein junction tight TJP2 lineage leukemia (trithorax (trithorax leukemia lineage 4 homolog, grainyhead- (Drosophilia) homolog ecdysoneless (Drosophila) RNA binding motif protein 13 cell division cycle associated 2 myeloid/

160 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3894995 chr20 - 2369715 2399499 5.23 3426917 chr12 + 94391437 94696442 5.23 3783749 chr183256689 + chr103961842 27925835 chr22 +3846594 28030948 5.26 - 89598814 chr19 89722145 39969442 5.25 - 40028027 5.24 3990713 4033507 5.24 2647742 chr3 + 151747168 151788822 5.27

30 (continued) 2A // 2A ’ // ’ // B 4 // MGC8758 // MGC8758 4

35 1 // FBI1 // LRF COD // SNRPB1 // // COD SmB/SmB snRNP- MNPEP // p67 // p67 // MNPEP // - p67elF2 -HSD- STRIN NARF // // // MGC11227 // BZS MHAM// MMAC1 // 2515369TEP1 // PTEN1 // KIAA1835 // Fug1 chr2 SD // MGC20266 // DKFZp5470146 FBI- + // MGC99631 // ZBTB7 // pokemon 172487173 172556842 5.26 CDA02 // EIF- // CDA02 // MST089 // MSTP004 MSTP089 40 003091 003091 006838 006838 016271 016271 003642 000314 002883 015898 032025 NM_ // NM_ 198216 NM_ // NM_ 018382 NM_ // NM_ 198128 NM_ // 001033085 NM_

45 SNRPB PTENRANGAP1 NM_ NM_ ZBTB7A NM_ // METAP2 FLJ11292 EIF2A NM_

55 Gene NameGene Symbol Gene Accession Synonym small nuclear nuclear small ribonucleoprotein B1 B and polypeptides ring finger protein 138 protein finger ring tensin and phosphatase RNF138 in (mutated homolog advanced multiple 1) Ran GTPase cancers 1 protein activating BTB domain and finger zinc 7A containing methionyl aminopeptidase protein // hypothetical 2 FLJ11292 occludens 2) eukaryotic eukaryotic 2) occludens translation initiation factor 65kDa 2A, 1 acetyltransferase histone HAT1

161 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 ’ chr4 + 1842909 1953717 5.23 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2715076 2715076 3316344 chr11 + 822755 828824 5.23 3834089 9 chr1 + 46460006 46505508 5.22

30 (continued) 3 // RAPH // 3 //

35 AP5 // FLJ23286 // // FLJ23286 // KIAA1090 // NSD2 // MMSET // // TRX5 REIIBP WHS GP27 // MER2 // // MER2 GP27 PETA- // SFA1 TSPAN24 // FKBP9 MGC20531 E1B- E1BAP5 // // E1BAP5 FLJ12944 40 44732 007331 133331 133335 004357 139030 144733 144733 007040 NM_ // 001042424 NM_ // NM_ // 133330 NM_ // NM_ // 133334 NM_ // NM_ 133336 NM_ // 001039490 NM_ // NM_ // 139029 NM_ // NM_ 182827 NM_ // NM_ // 144734 NM_ // NM_

45 WHSC1 CD151 // CD151 FKBP9L HNRPUL1

50 like 1 like like

55 Gene NameGene Symbol Gene Accession Synonym Hirschhom syndrome syndrome Hirschhom heterogeneous nuclear nuclear heterogeneous U- ribonucleoprotein Wolf- 1 candidate CD151 molecule (Raph // FK506 group) blood 9- protein binding

162 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3835544 chr19 + 49408524 49433254 5.21 3887049 chr20 +3680583 43874662 chur16 438789943195296 5.22 - chr9 11835208 + 11852988 5.22 139202850 139204636 5.22 3696524 chr162801608 - chr5 67914755 + 67931014 5.20 10406824 10490959 5.20 3886050 chr20 + 41519932 41526301 5.21

30 (continued) 14 // VI //

35 96 - // MGC161655 // // MGC161655 - pHZ- UBCH10 // UBCH10 dJ447F3.2 // MRX30CDKN1A // // OPHN3 MRX47 // // bPAK // PAK3beta hPAK3 // // CSIG // DKFZP564M182 // MGC138433 L12 // MGC142259 // NA- // N14 NA14 - // DOR1 // // // DOR1 - FLJ22315 // KIAA0597 MARCH- B52 // MGC5045 // MGC5045 // B52 SRP55 40 81799 82490 // // 82490 003445 007019 007019 181801 181803 022341 022341 015659 003731 005885 006275 014254 HP10481 3419585 chr12 + 62440396 62489599 5.20 NM_ NM_ // NM_ 198089 NM_ // NM_ // NM_ // 181800 NM_ // NM_ // 181802 NM_ // NM_ 002578 NM_ // NM_ 032382

45 Mar NM_ RSL1D1 NM_ SSNA1 // ZNF227 NM_ ZNF155 UBE2C // UBE2C // PAK3 6- PDF // COG8 PDF // SFRS6 NM_

50 associated ring

55 conjugating ’s syndrome syndrome ’s Gene NameGene Symbol Gene Accession Synonym rich 6 rich serine- splicing factor, arginine/ factor, splicing ribosomal L1 domain L1 domain ribosomal 1 containing Sjogren 1 autoantigen nuclear // zinc 227 protein finger zinc 155 protein finger ubiquitin- // p21 E2C enzyme (CDKN1A)-activated kinase 3 membrane- 6 (C3HC4) finger transmembrane protein 5 protein transmembrane deformylase peptide TMEM5 // (mitochondrial) of oligomeric component 8 complex golgi NM_

163 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2359736 chr1 + 151872948 151885444 5.18 3942179 chr22 + 28609182 28762301 5.19 2587520 chr23484005 - chr13 174445149 174610682 + 5.20 30028543 30132897 5.20

30 (continued) DSP1 // DSP1 // 35 // 2 SSS1 // DKFZP547E1010 3051395 // MGC131924 RP1- // MGC86949 chr7pp7704 // 178F15.2 - - 54753676 54847174 3871730 5.19 chr19 - 61261349 61355028 5.18 FYVE- // KIAA0371 ZFYVE10 DKFZp68601631 // // DKFZp68601631 SPR- LOC160824 // C13orf22 // D13S106E // DKFZp781K2286 RP11- // FLJ32952 // 121019.1 bA121019.1

40 014302 006947 - 015607 2728224 chr4 + 57028214 57064596 5.19 021090 021090 153051 003111 005800 005381FLJ45706 // C23 2603460 chr2 - 232027713 232080578 5.19 NM_ 001002836 NM_ // 001012456 NM_ NM_ // NM_ // 153050 NM_ NM_ // 001017371 NM_ // -

45 SRP72 NM_ C1orf77 NM_ USPL1 NM_ MTMR3 SP3 // RP11- RP11- SP3 // 114G1.1

55 Gene NameGene Symbol Gene Accession Synonym signal recognition particle particle recognition signal 72kDa open 1 chromosome 77 frame reading 787 protein finger zinc ZNF787 Sec61 gamma subunit gamma Sec61 G SEC61 ubiquitin specific peptidase peptidase specific ubiquitin 1 like nucleolinmyotubularin related 3 protein NCL NM_ Sp3 transcription factor // // factor transcription Sp3 factor transcription Sp3 pseudogene

164 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2459971 chr1 - 2277954913728097 227828457 5.18 chr173730941 + chr17 525175832452049 52667254 + chr1 5.18 592585232922215 59263555 - chr6 5.18 202639152 202647598 + 5.17 114284762 114292853 5.17

30 (continued)

35 // L // FLJ14368 PAF65B // PAF65B HSA276359 // AKAP // AKAP121 // AKAP149 D- // AKAP84 MGC1807 // AKAP1 PRKA1 // // SAKAP84 // // SUG1 S8 // TRIP1 // TBP10 // p45/SUG p45 C2- // FLJ14744 // P13K DKFZp686G16234 80K- // MACS FLJ90045 // MRACKS // // PRKCSL PKCSL 40 014409 004532 032833 001240 CYCT1 CCNT // 3453218 003488 chr1 2 - 002805 47372840 47397048 5.18 002356 NM_ // 001025247 NM_ XM_ // // 001125749 NM_ // NM_ NM // 018406 138297 NM_ // NM_ 002646

45 AKAP1 NM_ PSMC5 NM_ TAF5L // // TAF5L MUC4 // PPP1R15B PIK3C2B MARCKS NM_

50 rich rich kinase, kinase, 3- associated associated

55 Gene NameGene Symbol Gene Accession Synonym like RNA polymerase TAF5- p300/CBP- 11. cyclin T1 (PRKA) anchor A kinase 1 protein CCNT1 (prosome, proteasome subunit, 26S macropain) 5 ATPase, NM_ 1, phosphatase protein (inhibitor) regulatory // 15B subunit phosphoinositide- alanine- myristoylated factor (PCAF)-associated (PCAF)-associated factor cell 4, // mucin 65kDa factor, surface associated polypeptide 2, beta class substrate C kinase protein

165 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3005332 chr7 + 65131004 65262097 5.15 2553576 chr2 - 55051075 55161279 5.15 2423422 chr12328465 chr1 - + 93790445 94085633 32212249 5.15 32299034 5.15 2327630 chr1 + 28935740 28968859 5.15

30 A // (continued) REN- CL // C A // RCP // 35 CGRP- CRCP // CRCP // RCP // MGC111194 ASY // NI220/250 // // // NI220/250 ASY NOGO // NOGO- NSP // NSP- NSP // // Nbla00271 RTN- // Nbla10545 RTN4- X // // RTN4- B1 RTN4- // RTN4- B2 HGRG8 // NY- HGRG8 // // NSP2 KIAA0554 SH2D3B // Sam68 FLJ34027 p62 // 2

40 014478 007008 007008 153828 207521 005791 // MPP10P MPP10 145254 2488078 FLJ37611 016258 chr2 003567 3699581 + 006559 chr16 71210952 71237711 - 5.16 74034456 74107659 5.15 NM_ // 001040647 NM_ // 001040648 NM_ NM_ // NM_ // 020532 NM_ // NM_ // 207520 NM_ NM_

45 RCP9 YTHDF2 NM_ KHDRBS1 NM_ BCAR3 NM_ MPHOSPH1 0

50 estrogen related related

55 receptor Gene NameGene Symbol Gene Accession Synonym phase phosphoprotein phosphoprotein phase calcitonin gene- calcitonin peptide- protein component transmembrane protein 170 protein transmembrane TMEM170 family, YTH domain member 2 NM_ RNA containing, domain KH transduction signal binding, associated 1 4reticulon RTN4 resistance 3 resistance breast cancer anti- cancer breast M- nucleolar small (U3 10 ribonucleoprotein)

166 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3470689 chr123014742 chr7 -3707759 108010254 + chr17 108015656 5.13 98844221 + 98855171 5.13 5330450 5334853 5.13 3333711 chr11 +3331433 62380117 chr11 62412872 5.15 2438042 + chr1 57192053 57225319 - 5.14 154485643 154519254 5.14

30 5 (continued) RP1 // 35 // // EDG2 2 ABH2 // MGC90512 MGC90512 // ABH2 hABH2 // EDG- // MGC111202 G10 YCR063W // // 2510025F08Rik // KNTC2AP // MTW1 MGC2488 hMis12 // 4F2 // 4F2HC // 4F2HC // 4F2 // CD98 // 4T2HC // MDU1 // CD98HC NACAE // DKFZP586K0524 // KIAA1748 ZNF375 // EST1B FLJ34864 // KIAA1089 // LPTS- RP11- // LPTSRP1 54H19.7 // SMG-

40 003910 024039 001 002394 015457 015327 NM_ 001001655 NM_ // 001012661 NM_ // 012662 NM_ // 001012663 NM_ // 001012664 NM_ // 001013251 NM_

45 BUD31 NM_ MIS12 NM_ ZDHHC5 NM_ SMG5 NM_ ALKBH2 SLC3A2

50 type type

55 Gene NameGene Symbol Gene Accession Synonym 5 homolog, nonsense nonsense homolog, 5 BUD31 homolog (S. homolog BUD31 cerevisiae) kinetochore MIND MIS12, complex component, (yeast) homolog zinc finger, DHHC- zinc finger, 5 containing Smg- decay mRNA mediated (C. elegans) factor repair alkylation alk8, (E. coli) 2 homolog solute carrier family 3 family carrier solute and of dibasic (activators acid amino neutral 2 member transport),

167 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3876645 chr20 +2407439 11722386 chr1 118552393458033 5.12 chr12 - - 38195241 38229180 55318243 5.11 55326110 5.11 3299255 chr10 - 89500784 89591413 5.12 2948259 chr6 - 30260217 30290029 5.13

30 (continued)

35 KIAA0952 // // KIAA0952 // MGC130038 // 130039 MGC dJ742J24.1 // // PRPF9 PRP9 SF3a60 // SAP61 // // ATPSB ATPMB MGC5231 - // FSG1- FLJ14600 // AFDC1 FNP001 // 2756029 chr4 + 191051868 191138306 5.13 AFP // RNF95 // // // RNF95 AFP ZNF173 40 014962 014962 207350 207350 004599 SREBP2 006802 3947123 001686 chr22 + 40559049 40633247 5.12 032810 003449 NM_ // NM_ 181443 NM_ // NM_ 004477

45 SREBF2 NM_ SF3A3ATP5B NM_ NM_ ATAD1 NM_ BTBD3 MGC72104 // MGC72104 FRG1

50 containing 26 containing TRIM26 NM_

55 Gene NameGene Symbol Gene Accession Synonym sterol regulatory element element regulatory sterol factor transcription binding 2 3, subunit 3a, factor splicing 60kDa H+ synthase, ATP mitochondrial transporting, beta complex, F1 polypeptide ATPase family, AAA family, ATPase 1 containing domain BTB (POZ) domain 3 containing tripartite motif- tripartite protein FRG1 to similar 1 gene region (FSHD region FSHD // protein) 1 gene

168 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3351385 chr11 +3328214 117811029 chr11 117902749 5.10 + 43858633 43898486 5.10 2459438 chr1 - 226360734 226367172 5.11

30 1 // 1 (continued)

35 // // CXXC7 1 ALL- // HTRX1 HRX // // MLL/GAS7 TRX1 // MLL1A // DEPC- ABH3 // DEPC1 // MGC118790 // MGC118792 KIAA1625 3063083 chr7 - 98449133 98579664 5.11 AAVG5835 // AAVG5835 // DKFZp686D1387 // MGC61802 PRO19675 40 020429 020429 005933 152832 MTVR1 139178 3335338 chr11 + 65096490 65098230 5.10 181441 181441 181455 181462 181464 NM_ // NM_ 181349 NM_ // NM_ // 181454 NM_ // NM_ // 181456 NM_ // NM_ // 181463 NM_ // NM_ 181465

45 MLLFAM89B NM_ NM_ ALKBH3 NM_ SMURF1 MRPL55

55 or mixed- lymphoid Gene NameGene Symbol Gene Accession Synonym lineage leukemia (trithorax (trithorax leukemia lineage Drosophila) homolog, sequence with family 8 member 89. similarity repair alkylation alkB, (E. coli) 3 homolog myeloid/ SMAD specific E3 ubiquitin E3 ubiquitin specific SMAD 1 ligase protein mitochondrial ribosomal ribosomal mitochondrial L55 protein

169 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2839671 chr5 + 167845940 167878885 5.08 3833291 chr192901913 + chr6 451687722830638 45179181 chr5 + 5.08 30795977 + 30801165 5.08 137542289 137552275 5.08 2672532 chr3 - 47032936 47180418 5.09

30 1 // (continued) 56 // cl.

35 ArgRS // DALRD1 // DALRD1 // ArgRS MGC8641 MGC13687 // // MGC13687 // MGC23214 // MGC8570 S6 // // MIP224 TBP7 MGC117247 // M40 // MGC16435 // OK/SW- TUBB5 // TUBB1 MKLP2 // FLJ21151 RAB6KIFL // FLJ16420 // // FLJ16420 // FLJ22472 // FLJ23184 // HIF- FLJ45883 HYPB // HSPC069 KIAA1732 //

40 006503 006503 002887 178014 005733 014159 030815 // PDRG C20orf126 3902609 006002 - chr20 004712 - ZFYVE8 HRS // 3738138 29995826 3494102 chr17 30005314 chr13 5.09 + + 77260785 77279549 75021620 75078250 5.08 5.08 NM_ // NM_ 153001

45 PDRG1UCHL3 NM_ NM_ HGS NM_ PSMC4 50 terminal terminal

55 Gene NameGene Symbol Gene Accession Synonym tRNA synthetase RARS NM_ tubulin, betatubulin, 20A member family kinesin KIF20Aarginyl- TUBB NM_ NM_ SET domain containing 2 containing domain SET SETD2 DNA damage p53 and 1 regulated NM_ carboxyl- ubiquitin (ubiquitin L3 esterase thiolesterase) factor- growth hepatocyte kinase tyrosine regulated substrate (prosome, proteasome subunit, 26S macropain) 4 ATPase,

170 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3853942 chr19 -2478748 chr2 16489710 165171132434159 + 5.06 chr13818732 42250017 chr19 - 42418636 5.06 + 148161628 148167125 7319892 5.05 7443363 5.05 3683018 chr16 - 18700121 18709175 5.07 2382117 chr1 + 221955990 222031806 5.08

30 (continued)

35 DAN16 // SCAF6 // SCAF6 // // DAN16 // // CRSP70 SRA1 MED26 // C2orf2 DKFZp686P18118 // ELP120 // // FLJ10942 // FLJ32318 ROPP120 // MGC10828 SF3b49 // SAP49 // KIAA0521 MGC15913 FLJ27457 // // FLJ27457 // MGC111208 S15a CANPL2 // CANPml CANPml // CANPL2 // FLJ39928 // mCANP 40 006387 006387 001019 001019 019063 005850 015318 014303 PES 3957445 chr22 - 29302623 29333107 5.05 007027 TOP2BP1 2695941 chr3 - 134799729 134863527 5.07 001748 NM_ // NM_ 004831 NM_ // NM_ 001030009

45 EML4 NM_ SF3B4ARHGEF18 NM_ NM_ PES1 NM_ TOPBP1 NM_ CHERP // CRSP7 CAPN2 NM_

55 Gene NameGene Symbol Gene Accession Synonym echinoderm microtubule microtubule echinoderm associated protein like 4 4, subunit 3b, factor spicing 49kDa nucleotide guanine rho/rac 18 (GEF) factor exchange 1, homolog pescadillo domain BRCT containing (zebrafish) topoisomerase (DNA) II (DNA) II topoisomerase 1 protein binding homeostasis calcium reticulum endoplasmic required cofactor // protein transcriptional Sp1 for 7, 70kDa subunit activation, calpain 2, (m/II) large subunit S15a protein ribosomal RPS15A

171 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3315952 chr11 +2934089 chr6 550321 554016 + 5.05 160066607 160097332 5.04 2434925 chr1 - 149530589 149567792 5.03 3203311 chr9 - 32962360 33015096 5.03 2892979 chr6 + 4651344 4900768 5.03 3065963 chr7 - 103553146 103719295 5.04

30 HIT HIT (continued) BETA // 35 C11orf13 // HRAS1 // HRAS1 C11orf13 HRC1 // // // MGC126069 MGC126070 DKFZp686F20131 // KIAA0105 // - // MGC3925 P14K- // PI4KIIIbeta - // PI4Kbeta // FLJ20157 // FLJ20157 // MGC1072 CDYL1 // CDYL1 // DKFZP586C1622 MGC131936 AOA1 // AOA // // // EAOH AXA1 FHA- EOAHA // ORC5 // ORC5P // ORC5P // ORC5 ORC5T 40 004906 004906 152858 002651 002651 004824 004824 017692 175071 002553 002553 003475 NM_ // NM_ // 152857 NM_ // NM_ 005891 NM_ // NM_ // 000449 NM_ 001025603 NM_ // NM_ NM // 170751 170752 NM_ // NM_ // 175069 NM_ // NM_ NM // 175072 175073 NM_ 181747 NM //

45 RASSF7 NM_ WTAP // ACAT2 PIK4CB // RFX5 CDYL ORC5L 50 Coenzyme Coenzyme 6) domain 6) domain

55 (yeast) like Gene NameGene Symbol Gene Accession Synonym Wilms tumor 1 associated associated 1 tumor Wilms // acetyl- protein origin recognition complex, 5- subunit A acetyltransferase 2 A Coenzyme (acetoacetyl thiolase) family 7 family Ras association association Ras (RalGDS/AF- phosphatidylinositol 4- phosphatidylinositol beta catalytic, kinase, regulatory // polypeptide HLA X, 5 (influences factor II expression) class aprataxin APTX like chromodomain protein, Y- protein, chromodomain

172 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 2336271 chr1 + 52293292 52339895 5.01 3895075 chr20 - 2586736 2592862 5.01 3056044 chr7 - 72492710 72574552 5.01 2382336 chr13591963 chr15 + + 222368455 222416368 5.02 42616580 42644124 5.02 3017547 chr7 + 104436029 104542698 5.02 3573152 chr4 - 77042100 77202740 5.02

30 (continued)

35 // elF3- alpha MGC23908 // // MGC23908 RP4- // MGC88389 800M22.5 FLJ11043 // H- // FLJ11043 // MGC903 IDHB WBSCR10 // // WBSCR10 WSTF // WBSCR9 FLJ10766 // Fbx28 Fbx28 // FLJ10766 KIAA0483 // elF3- // elF3j p35 FLJ10078 // // FLJ10078 // FLJ14026 HDCMC04P // MGC70452 KIAA0526 // LCB2 // // LCB2 KIAA0526 SPT2 40 152265 006899 006899 174856 023005 023005 018682 018682 015176 003758 006468 // RPC62 RPC3 2432647 chr1 - 144297192 144333220 5.01 004863 NM_ // NM_ // 174855 NM_ NM_ // NM_ 032408 NM_ // NM_ 182931

45 BTF3L4 NM_ IDH3B EIF3S1 NM_ POLR3C NM_ BAZ1B MLL5 SPTLC2 NM_ CDCA5 NM 080668 MGC16386 3377423 chr11 - 64592075 64608249 5.02

55 or mixed- lymphoid Gene NameGene Symbol Gene Accession Synonym box protein 28 protein box FBXO28 NM_ like 4 like basic transcription factor 3- factor transcription basic isocitrate dehydrogenase 3 dehydrogenase isocitrate (NAD+) beta eukaryotic translation translation eukaryotic 1 3, subunit factor initiation 35kDa alpha, (RNA) III (DNA polymerase C polypeptide directed) (62kD) bromodomain adjacent to 1B domain, finger zinc F- lineage leukemia 5 5 leukemia lineage (trithorax homolog, Drosophila) serine serine palmitoyltransferase, long 2 subunit base chain cell division cycle associated 5 myeloid/

173 EP 2 136 209 A1 Fold Fold Change 5

15 Strand Start Stop Human Genome hg18 Genome Human

20 some Chromo Chromo

25 Human Exon ST Exon ST 1.0 Array 1.0 Transcript Transcript ID Cluster 3205659 chr9 - 37901375 38059198 5.00

30 (continued)

35 RP11-3J10.8 // // bA3J10.2 // LB1 // FLJ10749 TMAP // se20-10 // // CG7943

40 003028 003028 033412 NM_ // NM_ // 018204 NM_

45 SHB // CKAP2 SHB // // MCART1

55 Gene NameGene Symbol Gene Accession Synonym Src homology 2 domain protein adaptor containing associated B // cytoskeleton // mitochondrial 2 protein 1 repeat triple carrier

174 EP 2 136 209 A1

Example 9: Analysis with microarray (3)

[0176] Using the PBMC samples in Example 4(2), genes of which introns exhibited increased expression were identified. Ribosomal RNA was removed from 1 Pg of each total RNA of control cells (n=3) and cells with the treatment (n=3) 5 using RiboMinus Human/Mouse Transcriptome Isolation Kit (Invitrogen). Single stranded cDNA synthesis, double stranded cDNA synthesis, cRNA synthesis, second single stranded cDNA synthesis, cDNA fragmentation, and cDNA labeling in order were carried out for total RNA from which ribosomal RNA was removed, using GeneChip Whole Transcript Sense Target Labeling and Control Reagents (Affymetrix) to make a cDNA probe. Subsequently, the cDNA probe was used for hybridization with Human Exon 1.0 ST Array (Affymetrix). The array was washed and stained, and luminescence 10 intensity was measured by a scanner. [0177] The expression level of the probe set and the gene was quantified by using Expression Console Ver. 1.0 (Affymetrix) with Summarization Method and Normalization Method being set to "Median polish as used in RMA" and "None", respectively. The expression level of the probe was normalized with that of the gene.

15 (1) Identification of a gene of which introns exhibit increased expression in a group with the treatment at a concentration of 3 nM

[0178] Probe sets showing that the normalized change in the level expression of the probe set in the group with the treatment at 3 nM was more than 5 times; the expression level of the probe set and the gene in the group with the 20 treatment at 3 nM was more than 100; and probe set annotation was "extended, full, free", were picked out. Welch’s t- test was conducted with the probe sets extracted for the group with the treatment at 3 nM and the control group to determine a p value and a q value. A gene containing the probe sets with the q value of less than 5% was determined as a candidate gene with increased expression level of the intron regions (Table 4). [0179] In Table 4, for the gene evaluated, gene name (Gene Name), abbreviated name (Gene Symbol), accession 25 number (Accession), alias name (Synonym), transcription cluster number in Human Exon 1.0 ST Array (Human Exon 1.0 ST Array Transcript Cluster ID), chromosome number (Chromosome), type of strand (Strand), start region (Start), stop region (Stop), and change in expression level (Fold Change) were respectively shown.

175 EP 2 136 209 A1

5 Fold Change Fold

25 hg18 Genome Human someChromo Strand Start Stop

30 3556888 chr14 - 22439714 22458231 7.63 2939034 chr6 - 2832402 2858242 7.75 3959451 chr22 - 35007278 35113982 7.90 3227696 chr9 - 133441988 133605262 9.27 2883440 chr5 - 156755122 156935351 9.71 Human Exon Exon Human 1.0 ST Transcript ID Cluster 3976341 chrX + 47326654 47332978 14.98 [Table 4] [Table

35 A // II- 3 // CAP3 // CAP3 // 3 // CAPERbeta // CAPERbeta // FLJ10482 // MGC4458 RNPC4 // PP239 CAP- CAP // PI9 // DKFZp686I0422 // // MGC111370 2 // MSTP057 DFNA17 // EPSTS EPSTS // DFNA17 // // MHA // FTNS NMHC- NMMHCA C3G // C3G DKFZp781P1719 // GRF2 FKSG34 // FKSG34 MADDAM // MLTNB CLGI // EPA // CLGI // // FLJ90373 EPO // TIMP // HCl

40 0010773 0010773 018107 004155 // 004155 004568 002473 006202 PDE4 // DPDE2 3820501 // 005312 198679 chr19 + 10388560 10451531 9.64 023038 // 023038 033274 003254 NM_ // NM_ 51 // 52 0010773 NM_ NM_ NM_ NM_ NM_ NM_ NM_

45 RBM23 SERPINB9 // SERPINB9 // SERPINB6 MYH9 NM_ PDE4A NM_ RAPGEF1 ADAM19 50 TIMP1 NM_ specific specific 55 muscle RNA binding motif 23 protein serpin peptidase B clade inhibitor, (ovalbumin), serpin 9 // member inhibitor, peptidase B (ovalbumin), clade member 6 myosin, heavy chain chain heavy myosin, non- 9, phosphodiesterase phosphodiesterase cAMP- 4A, (phosphodiesterase homolog, E2 dunce guanine Rap nucleotide factor exchange (GEF) 1 Gene Name GeneSymbol Accession llopeptidase ADAM (meltrin 19 domain Synonym beta) TIMP TIMP metallopeptidase 1 inhibitor

176 EP 2 136 209 A1

5 Fold Change Fold

20 Human Genome hg18 Genome Human 25 someChromo Strand Start Stop

30 Human Exon Exon Human 1.0 ST Transcript Transcript ID Cluster 2704894 chr3 - 171287994 171381537 7.30 3430462 chr12 + 106237825 106577543 7.07 3326183 chr11 + 34009711 34081946 6.78 3884191 chr203542847 chr14 + 35406502 + 35467847 6.98 70857592 71468470 6.93 (continued) Src 35 DKFZp313K1221 DKFZp313K1221 // // EDR3 // FLJ12729 HPH3 // FLJ12967 // MGC88144 ASV // SRC1 // c- SRC1 // ASV // SRC // p60- FLJ33957 // FLJ33957 FLJ42845 GPIP137 // GPIP137 // p137GPI M11S1 CD11C 3657041 chr16 + 31274012 31301819 6.76 DKFZp686G134 4 DKFZp686G134 // // E6TP1 KIAA0440

40 024947 005417 // 005417 198291 005066 PSF // POMP100 2406064 0010175 chr1 152322 - 35351696 35506894 7.08 007067// HBOA HB01 // 005898 203364 3725779 chr17 + 45196447 45261455 6.84 015556 0011278 0011278 NM_ NM_ NM_ // NM_ 23 // 72 0010180 NM_ XM_ // NM_ 69 000887 NM_ NM_

45 PHC3 NM_ SRC SFPQ NM_ BTBD11 ITGAX MYST2GPIAP1 NM_ 50 SIPA1L1 NM_

55 A- Ruppin glutamine- induced induced anchored anchored src sarcoma Gene Name GeneSymbol Accession Synonym splicing factor factor splicing proline/ polyhomeotic polyhomeotic 3 homolog (Drosophila) 2) viral oncogene oncogene viral 2) (avian) homolog v- (Schmidt- rich (polypyrimidine (polypyrimidine rich protein binding tract associated) BTB (POZ) domain BTB (POZ) domain 11 containing integrin, alpha X alpha integrin, (complement 3 component 4 subunit) receptor signal- proliferation- histone MYST 2 acetyltransferase GPI- membrane protein1 associated 1 like1

177 EP 2 136 209 A1

5 Fold Change Fold

20 Human Genome hg18 Genome Human 25 someChromo Strand Start Stop

30 3409081 chr12 + 27288343 27370157 5.97 2652410 chr3 + 173240112 173601176 5.97 3020192 chr7 +3186966 115637811 115743800 chr9 6.22 + 119506334 119670150 6.00 Human Exon Exon Human 1.0 ST 3362263 chr11 -2982381 9116953 chr6 9243468 6.61 - 160119521 160130731 6.19 Transcript Transcript ID Cluster 3882069 chr20 + 30871304 30901864 6.65 (continued) 2 //

35 alpha // alpha alpha KL4A0965 // KL4A0965 NDR2 DKFZp686D141 DKFZp686D141 70 // // DKFZp762K137 // FAD104 // FLJ23399 // MGC10002 // PRO4979 YVTM2421 DKFZP586B202 2 DKFZP586B202 // // MGC1146 TESS // TESS- CCT- CCTa // CCT1 // TCP- // D6S230E 1- // // TOLL CD284 hToll FLJ22354 // FLJ22354 // FLJ33829 // FLJ43455 KIAA1091 EB1 // EB1 // // MGC117374 MGC129946

40 015000 0010088 0010088 022763 015641 // 015641 152829 152272 MGC29816 138554 3089853 chr8 + 23157105 23176288 6.08 015213 012325 NM_ // NM_ 97 030752 NM_ NM_

45 STK38L NM_ FNDC3B NM_ TES CHMP7 NM_ RAB6IP1 NM_ 50 MAPRE1 NM_

55 threonine like receptor 4 receptor like TLR4 NM_ complex 1 TCP1 serine/ like 38 kinase t- III type fibronectin containing domain 3B Gene Name GeneSymbol Accession Synonym testis derived LIM (3 transcript domains) family, CHMP member 7 toll- RAB6 interacting RAB6 interacting 1 protein microtubule- protein, associated RP/EB family, member 1

178 EP 2 136 209 A1

5 Fold Change Fold

20 Human Genome hg18 Genome Human 25 someChromo Strand Start Stop

30 2855501 chr5 - 43324231 43349337 5.74 3377226 chr11 - 64376790 64404202 5.78 Human Exon Exon Human 1.0 ST 2345929 chr1 + 89871229 90008050 5.81 Transcript Transcript ID Cluster 2655688 chr3 + 185514970 185535829 5.83 3362719 chr11 -4027585 10487574 chrX 10788746 5.97 - 153658739 154075618 5.94 (continued)

35 6 // MGC1405 6 3033209 chr7 + 154649208 154732868 5.72 HMGCS // HMGCS MGC90332 CL- FLJ42622 // FLJ42622 // H- FLJ44618 HPAST1 PAST // // PAST1 // PAST AD158 // AD158 DKFZp5B6J1119 // // FAD158 MGC138551 DKFZp686A1451 DKFZp686A1451 // EIF4G // // EIF4F p220 AAG1 // DAP5 // // AAG1 // NAT1 FLJ41344 // p97 // PSA MP100 3724698 // DXS552 AAG12 // // DXS552E // // MRG1 EMP55 chr17PEMP + 42955347 43057168 5.96

40 005542 // 005542 // 198336 002130 006795 032270 0010425 0010425 // 004953 // 182917 // 198241 // 198242 198244 002436 0011285 0011285 NM_ NM_ NM 198337 NM_ // NM_ 59 001418 XM_ // NM_ 88 006310 NM_ NM_ NM_ NM_ NM_

45 INSIG1 HMGCS1 NM_ EHD1 NM_ LRRC8C NM_ EIF4G2 NPEPPS EIF4G1 50 MPP1 NM_ 3- 55 domain domain hydroxy- insulin induced gene gene induced insulin 1 3- methylglutaryl- Coenzyme A 1 (soluble) synthase Gene Name GeneSymbol Accession Synonym EH- 1 containing leucine rich repeat repeat rich leucine 8 family, containing member C eukaryotic eukaryotic translation initiation factor 4 gamma, 2 aminopeptidase sensitive puromycin eukaryotic translation initiation factor 4 gamma, 1 membrane protein, 1, palmitoylated 55kDa

179 EP 2 136 209 A1

5 Fold Change Fold

20 Human Genome hg18 Genome Human 25 someChromo Strand Start Stop

30 3482498 chr13 + 25701360 25877335 5.53 4009315 chrX - 53575796 53740871 5.54 2674242 chr3 - 49371587 49424514 5.54 2771718 chr4 - 68130308 68249472 5.57 Human Exon Exon Human 1.0 ST Transcript Transcript ID Cluster 3896370 chr20 - 5473033 5546357 5.68 3960629 chr22 - 37202800 37232288 5.70 (continued)

35 BP1 // 10 // LYT10 // 10 3261643 chr10 + 104144262 104152716 5.61 K35 // // MGC126074 MGC126075 ARF- HECTH9 // Ib772 // HSPC272 // // KIAA0312 // // MULE LASU1 ARH12 // ARHA // RHO12 // FLJ10808 // FLJ10808 FLJ23367 LYT- FLJ11085 // FLJ11085 // K1AA1434 MGC26147 DKFZp781D172 7DKFZp781D172 3609138 DKFZp761H2016 chr15 RH70 // // P72 + 91227096 91387351 5.70

40 001260 031407 001664 018227 0010774 0010774 002502 0010425 0010425 019593 006386 // 006386 030881 NM_ // NM_ 93 // 94 0010774 NM_ NM_ // NM 72 001271 NM_ NM_

45 CDK8 NM_ HUWE1 NM_ RHOA NM_ UBE1L2 NM_ NFKB2 CHD2 RP5-1022P6.2 NM_ 50 DDX17 Ala- cells 2 cells Glu- like 2 like

55 activating dependent dependent cyclin- kinase 8 HECT, UBA and UBA and HECT, domain WWE 1 containing ras homolog gene gene homolog ras A member family, Gene Name GeneSymbol Accession Synonym ubiquitin- E1- enzyme nuclear factor of factor nuclear light kappa gene polypeptide B- in enhancer (p49/p100) chromodomain DNA helicase 2 protein binding protein hypothetical KIAA1434 DEAD (Asp- Asp) box box Asp) 17 polypeptide

180 EP 2 136 209 A1

5 Fold Change Fold

20 Human Genome hg18 Genome Human 25 someChromo Strand Start Stop

30 3819543 chr19 + 8415651 8459993 5.34 Human Exon Exon Human 1.0 ST 3068097 chr7 - 111152902 111633744 5.42 Transcript Transcript ID Cluster 3147321 chr8 - 103333634 103493671 5.49 3253880 chr10 + 80777230 80785093 5.19 3504434 chr13 - 20251014 20375187 5.33 2326448 chr1 + 26478669 26480591 5.34 (continued) D //

35 1 // TIP- 1 SH3BP- DKFZp547H118 // // DKFZp547H118 HNRNPM // HNRNPM4 // HNRPM4 // NAGR1 HTGR1 // FLJ34238 // FLJ34238 // KIAA0716 // MGC134911 MGC134912 DD5 // EDD // DD5 // // HYD FLJ11310 // // KIAA0896 MGC57263 FLJ90798 // FLJ90798 MGC117207 CYP3 // Cyp- CYP3 // FLJ13046 // FLJ13046 KIAA1721 B1 // B1 // 7 DKFZP434L011 // DKFZp434P232 // // FLJ13976 FLJ22000

40 031286 // 031286 022778 004599 SREBP2 // 005968 031203 3947123 chr22 + 40559049 40633247 5.40 014705 015902 003129 005729 3114832 chr8 + 126063738 126105522 5.19 022459 NM_ NM_ NM_ NM_

45 SH3BC3RL3 // SH3BC3RL3 // CCDC21 SREBF2 NM_ HNRPM DOCK4 NM_ EDD1 NM_ 50 PPIF NM_ rich

55 coil domain SH3 domain binding binding domain SH3 glutamic acid- // 3 like protein coiled- 21 containing Gene Name GeneSymbol Accession Synonym regulatory sterol binding element 2 factor transcription heterogeneous nuclear M ribonucleoprotein dedicator of of dedicator 4 cytokinesis E3 ubiquitin protein protein ubiquitin E3 HECT ligase, 1 containing, domain squalene epoxidasesqualene SQLE peptidylprolyl F isomerase F) (cyclophilin NM_ exportin 4exportin XPO4 NM_

181 EP 2 136 209 A1

5 Fold Change Fold

20 Human Genome hg18 Genome Human 25 someChromo Strand Start Stop

30 Human Exon Exon Human 1.0 ST 2478748 chr2 + 42250017 42418636 5.02 Transcript Transcript ID Cluster 2500550 chr2 + 112372656 112513624 5.12 (continued)

35 C2orf2 // C2orf2 DKFZp686P1811 // ELP120 8 // // FLJ10942 // FLJ32318 ROPP120 MER // // MER c- // MGC133349 mer

40 019063 003131 MCM1 006343 2907730 chr6 + 43246765 43257189 5.15

45 EML4 NM_ 50 SRFMERTK NM_ NM_

55 serum fos mer proto- mer Gene Name GeneSymbol Accession Synonym echinoderm echinoderm microtubule protein associated 4 like serum response response serum (c- factor response element- transcription binding factor) c- tyrosine oncogene kinase

182 EP 2 136 209 A1

(2) Identification of the gene of which introns exhibit increased expression in a dose-dependent fashion in groups with the treatment at a concentration of 3 nM, 10 nM, and 30 nM.

[0180] Probe sets showing that the normalized change in the level expression of the probe set in the group with the 5 treatment at 30 nM was more than 5 times; the expression level of the probe set and the gene in the group with the treatment at 30 nM was more than 100; and probe set annotation was "extended, full, free", were picked out. Regression analysis was performed with the probe sets extracted for the control group, the group with the treatment at 3 nM, the group with the treatment at 10 nM, and the group with the treatment at 30 nM to determine a p and q value for the slope of regression formula. A gene containing the probe sets with the q value of less than 5% was determined as a candidate 10 gene with increased expression level of the intron regions (Table 5). [0181] In Table 5, for the gene evaluated, gene name (Gene Name), abbreviated name (Gene Symbol), accession number (Accession), alias name (Synonym), transcription cluster number in Human Exon 1.0 ST Array (Human Exon 1.0 ST Array Transcription Cluster ID), chromosome number (Chromosome), type of strand (Strand), start region (Start), stop region (Stop), and change in expression level per 1 nM (Fold Change/nM) were respectively shown. 15

183 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3976341 chrX + 47326654 47332978 1.08 3772525 chr17 - 74181731 74289973 1.08 3908963 chr20 - 47682889 47809709 1.08 3225398 chr92981912 - chr6 127038953 - 127064590 1.08 159106770 159160432 1.08 2519229 chr2 + 187163045 187253869 1.08 2556302 chr2 - 64173290 64225291 1.08 Transcript Transcript ID Cluster Human ST Exon 1.0

30 1 // V // gt- [Table 5] [Table T5 // T5 // T5 // BETA4- // T5 N // CLGI // EPA // EPO EPA // // CLGI // FLJ90373// HCI // TIMP B2-1 // // B2-1 CYTOHESIN- // D17S811E // FLJ34050 // SEC7 FLJ41900 B4Gal- GALT- // MGC138470 beta4Gal- beta4GaIT- BIP // FLJ26106 // // FLJ26106 BIP MIF2 // GRP78 CVL // // CVIL // DKFZp762H157 // FLJ26216 MGC1584 CD51 // MSK8 // MSK8 // CD51 VNRA 35 DKFZp686C18116 MGC50990 // 003254 004762 139265 PAST4 3620276 chr15 - 39977674 40052063 1.08 004776 005347 003379 002210 001432 ER 020651 2731513 chr4 + 75440309 75473341 1.08

40 NM_ // NM_ 017456

45 TIMP1 NM_ PSCD1 B4GALT5 NM_ HSPA5 NM_ ITGAV NM_

50 (cytohesin (cytohesin betaGlcNAc beta 1,4- beta betaGlcNAc 55 protein, regulated coil domains 1 Gal: domain containing 4 containing domain EHD4 NM_ EH- TIMP metallopeptidase inhibitor inhibitor metallopeptidase TIMP 1 1) pleckstrin homology, Sec7 and and Sec7 homology, pleckstrin coiled- villin 2 (ezrin) villin UDP- galactosyltransferase, 5 polypeptide VIL2 NM_ heat shock 70kDa protein 5 protein 70kDa shock heat (glucose- 78kDa) integrin, alpha V (vitronectin V (vitronectin alpha integrin, polypeptide, alpha receptor, CD51) antigen pellino homolog 1 (Drosophila) homolog pellino PELI1 NM_ epiregulin EREG NM_ Gene Name Gene Symbol Accession Synonym

184 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3362263 chr11 - 9116953 9243468 1.07 2876046 chr5 - 133557588 133589841 1.07 3218528 chr9 - 106583121 106748222 1.08 2581548 chr2 - 153212414 153283546 1.08 Transcript Transcript ID Cluster 2501204 chr2 + 113573383 113608060 1.08 Human ST Exon 1.0

30 REN- (continued) 1 // ABC1 // 1 // 11 // FBP11 // // FBP11 11 1RA // IL- 1ra3 // IL- 1ra3 1RA C KIAA0571 3383227 chr11 - 77603886 77989843 1.07 FLJ22354 // FLJ22354 // FLJ33829 // FLJ43455 KIAA1091 PP2Ac // PP2CA // // PP2CA PP2Ac RP- ABC- // FLJ14958 CERP // TGD HDLDT1 // FBP- FLJ20585 // FLAF1 // HIP10 FNBP3 // // // NY- HYPA 35 ICIL- // // IL1RA IL1F3 // // MGC10430 IRAP 012296 173496 FLJ32798 015213 3282601 chr10 - 28377816 28631969 1.07 002715 005502 000577 173842 371575 371575 NM_ // NM_ 080491 XM_ // XM_ 938514 40 NM_ // NM_ // 173841 NM_ // NM_ 173843

45 GAB2 MPP7 NM_ RAB5APPP2CA 004162 NM RAB5 NM_ 2613386 chr3 + 19963571 20002852 1.07 ABCA1 NM_ PRPF40A

50 mRNA processing processing mRNA

55 associated binding binding cassette,sub- GRB2- 2 protein RAB6 interacting protein 1 protein RAB6 interacting RAB6IP1 NM_ membrane protein, p55 (MAGUK 7 palmitoylated 7) member subfamily RA85A, member RAS RAS member RA85A, family oncogene (formerly 2 phosphatase protein 2A), catalyticsubunit, alpha isoform ATP- family A (ABC1), member 1 member A (ABC1), family interleukin 1 receptor antagonist receptor 1 interleukin IL1RN pre- PRP40 A (S. homolog 40 factor cerevisiae) Gene Name Gene Symbol Accession Synonym

185 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3497270 chr13 + 95125276 95245596 1.07 3975869 chrX + 46581319 46637601 1.07 2922215 chr6 + 114284762 114292853 1.07 3387259 chr113376155 - chr11 - 94545767 94605309 62316178 1.07 62329529 1.07 3738629 chr17 + 77775274 77812305 1.07 2633587 chr3 + 101462368 101526762 1.07 2325593 chr1 + 24943202 25071376 1.07 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) L // FLJ14368 // FLJ14368 // L HP58 // P58 // P58 // HP58 // PRKRI P581PK KlAA0215 // KlAA0215 TBCCD2 80K- // MACS FLJ90045 // MRACKS // // PRKCSL PRKCSL MGC29667 // MGC29667 SEST3 // DKFZp66700311 TAP // MEX67 MCT3 // MCT4 // // MCT4 MCT3 // MGC138472 MGC138474 DKFZp667G062 // // DKFZp667G062 // FLJ11046 NS4ATP1 35 // CUC4L // DKFZP566G223 // // H1 FLJ38640 // // p64H1 huH1 ADDL 006260 006915 002356 144665 006362 018309 013943 016824 NM_ // 001081491 NM_ NM_ // 001042422 NM_ // 001042423 004207 NM 40 NM_ // NM_ // 001121 NM_ // NM_ 019903

45 DNAJC3 NM_ RP2 NM_ MARCKS NM_ SLC16A3 TBC1D23 NM_ CLIC4 // ADD3 // CLIC4 linked linked 50 rich rich

55 DnaJ (Hsp40) homolog, 3 member C, subfamily retinitis pigmentosa 2 (X- 2 pigmentosa retinitis recessive) nuclear RNA export factor 1 factor export RNA nuclear NXF1 alanine- myristoylated protein kinase C substrate C kinase protein sestrin 3sestrin SESN3 NM_ solute carrier family 16, member member 16, family carrier solute acid 3 (monocarboxylic 4) transporter TBC1 domain family, member member family, domain TBC1 23 chloride intracellular channel 4 4 channel intracellular chloride 3 (gamma) adducin // Gene Name Gene Symbol Accession Synonym

186 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2803329 chr5 + 17118727 17381190 1.07 4035017 chrY - 13772846 14101944 1.07 2551924 chr2 - 47232159 47286178 1.07 3462094 chr12 - 70269806 70344289 1.07 2863730 chr52711644 - chr3 - 77318390 77671471 195604703 1.07 195757213 1.07 Transcript Transcript ID Cluster 2571483 chr23419849 chr12 - + 113247977 113259446 63132014 1.07 63202097 1.07 Human ST Exon 1.0

30 (continued) 23 // CAP23 // // // CAP23 23 1A // IL1 // IL1- // // IL1 1A CAP- NAP- // MGC8555 NAP22 // 22 DKFZp686L12190 DKFZp686L12190 // UTY1 // DKFZp686A03225 // MGC141941 // bA386N14.2 CAMII // PHKD // // PHKD CAMII PHKD2 DKFZp686A0722 // // DKFZp686A0722 // KIAA0546 // MGC23401 // MGC90200 PSRC2 ADTB3 // ADTB3A ADTB3 // PE // HPS2 HPS // AFURS1 DKFZp686K16189 // FLJ90613 35 IL- // ALPHA // // NAK FLJ11330 T2K 006317 007125 182660 001743 144982 003664 000575 013254 931948 931948 NM_ // NM_ // 182659 NM_ // NM_ 021140 40 XM_ // XM_ 942079

45 BASP1 NM_ UTY // UTX UTY CALM2 NM_ CCDC131 NM_ AP3B1 NM_

55 complex protein related binding kinase 1 kinase binding TBK1 NM_ coil domain containing linked // ubiquitously // ubiquitously linked brain abundant, membrane membrane abundant, brain 1 protein signal attached ubiquitously transcribed transcribed ubiquitously gene, repeat tetratricopeptide Y- transcribed tetratricopeptide X chromosome repeat, calmodulin 2 (phosphorylase delta) kinase, ATPase type 13A3 type ATPase coiled- 131 ATP13A3 3, beta 1 subunit 1 beta 3, TANK- adaptor- interleukin 1, alpha 1, interleukin IL1A NM_ Gene Name Gene Symbol Accession Synonym

187 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2480168 chr2 + 45731934 46343070 1.07 2796553 chr4 - 185913758 186002178 1.07 3565524 chr14 - 54375952 54439279 1.07 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 1 // 1 CH- MGC125656 // MGC125656 // MGC125657 // nPKC- PKCE epsilon ACS1 // FACL1 // FACL1 // ACS1 // // LACS FACL2 LACS2 // LACS1 S171 3571347 chr14 - 72811631 73000081 1.07 35 GCH // // DYT5 GTP- GTPCH1 005400 001995 003744 002809 S3 // RPN3 // P58 3720636 chr17 + 35390438 35407732 1.07 000161 NM_ // 001005743 NM_ // 001005744 NM_ // 001005745 NM_ 40 NM_ // NM_ // 001024024 NM_ // 001024070 NM_ 001024071

45 ACSL1 NM_ PSMD3 NM_ GCH1 chain chain 50

55 CoA synthetase long- numb homolog (Drosophila) homolog numb NUMB epsilon C, kinase protein PRKCE NM_ family member 1 member family acyl- proteasome (prosome, (prosome, proteasome non- subunit, 26S macropain) ATPase, 3 ATPase, GTP cyclohydrolase 1 (dopa- responsive dystonia) Gene Name Gene Symbol Accession Synonym

188 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3923257 chr21 + 43963416 44006601 1.07 3623424 chr15 - 47203877 47235198 1.07 2737717 chr4 + 103568522 103757506 1.07 3156193 chr8 - 141599440 141726037 1.07 2935475 chr6 + 163684268 163960462 1.07 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 1 // KBF1 // // KBF1 1 B // NFKB- B C21 orf97 // PKH // // PKH orf97 C21 // // FLJ31940 PNK // MGC15873 PRED79 ALIEN // CSN2 // // ALIEN // TRIP15 SGN2 DKFZp686C01211 DKFZp686C01211 EBP- // // NF- MGC54151 kappa- p105 // AGO2 // MGC3183 // MGC3183 AGO2 //Q10 35 // DKFZp58610923 // QK3 QK // Hqk 003681 004236 003198 TCEB3A // SIII 2325251 chr1 + 23942459 23961135 1.07 003998 012154 206853 206855 945803 945803 001767// T11 SRBC 2353669 chr1 + 117098550 117149098 1.07 NM_ // NM_ 032920

40 XM_ // NM_ // 006775 NM_ // NM_ // 206854 NM_

45 PDXK // C21orf124 COPS2 NM_ TCEB3 NM_ NFKB1 NM_ EIF2C2 NM_ QK1

55 pyridoxal(pyridoxine, vitamin 21 chromosome // kinase B6) 124 frame reading open COP9 constitutive constitutive COP9 homolog photomorphogenic 2 (Arabidopsis) subunit transcription elongation factor B (SIII), polypeptide 3 (110kDa, A) elongin CD2 molecule light of kappa factor nuclear in B- enhancer gene polypeptide cells 1 (p105) CD2 M_ eukaryotic translationinitiation 2 2C, factor quaking homolog, KH domain domain KH homolog, quaking (mouse) binding RNA Gene Name Gene Symbol Accession Synonym

189 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2948425 chr6 - 30676177 30694348 1.07 3233182 chr10 +2566414 chr2 5444535 - 5491001 1.07 98600132 98714000 1.07 3964154 chr22 -3980887 chrX 45454343 45537349 + 1.07 70420006 70437726 1.07 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) IV // GNT- IVA IVA GNT- // IV CAT53 // FB19 // // // FB19 CAT53 PNUTS ARHGEF8 // ARHGEF8 NET1A GNT- 6330578E17Rik // DKFZp434E02H // // DKFZp434E02H // FLJ21430 // FLJ23239 // LK4 // KIAA1646 // MGC131878 // dA59H18.2 // dA59H18.3 hCERK NRB54 // // NMT55 P54NRB // P54 35 NUP196 // ADIR2 3359910 chr11 - 3652836 3775353 1.07 002714 005863 012214 013255 FLJ11162 022766 3024275 chr7 + 007363 130445315 130837940 1.07 005387 139131 NM_ // 001047160 NM_ NM_ // NM_ 001008215 NM_ // NM_ 182661 40 NM_ // NM- // 016320 NM_ // NM_ 139132

45 PPP1R10 NM_ MGAT4A // MGAT4A MGC52110 NET1 MKLN1 NM_ NONO NM_ N-

50 1,4-

55 binding POU domain containing, containing, domain POU 1,3-)-glycoprotein beta- 1,3-)-glycoprotein mannosyl (alpha- mannosyl 1, phosphatase protein 10 subunit (inhibitor) regulatory acetylglucosaminyltransferase, acetylglucosaminyltransferase, // hypothetical A Isozyme MaC52110 protein non- octamer- transforming cell neuroepithelial 1 gene ceramide kinase CERK nucleoporin 98kDanucleoporin intracellular 1, muskelin motifs kelch containing mediator NUP98 Gene Name Gene Symbol Accession Synonym

190 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2431886 chr1 - 142444924 143804054 1.06 3970130 chrX + 16639861 16690708 1.06 3864551 chr19 -3751184 chr17 48841865 - 48866539 1.06 24256404 24302905 1.06 3272205 chr10 + 134201308 134446967 1.07 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) COAS3 // CMYA2 // // CMYA2 // COAS3 // DKFZp781J054 // MGC75440 MMGL DKFZp686K221 // DKFZp686K221 // FLJ14495 // FLJ44185 PRO3113 CD87 // UPAR // // CD87 URKR KIAA1523 PF1 // MGC131914 35 // 5PTASE // DKFZp434A1721 // MGC116947 MGC116949 001 014644 032796 002659 005539 003242 003242 NR_ // XM_ // 943179 NM_ // 002810 NM_ 001D02811 // NM_ // 001002812 NM_ // NM_ 022359 NM_ // 001005376 NM_ // 001005377 NM_ NM_ // 001033561 020889 NM 40 XM_ // 001133189 NM_

45 Clorf152 // Clorf152 PDE4DIP SYAP1 NM_ PLAUR INPP5A

50 5-

55 chromosome 1 open reading reading open 1 chromosome // phosphodiesterase 152 frame protein interacting 4D (myomegalin) PHD finger protein 12 protein finger PHD 1, protein associated synapse PHF12 (Drosophila) homolog SAP47 plasminogen activator, activator, plasminogen receptor urokinase inositol polyphosphate- phosphatase, 40kDa phosphatase, Gene Name Gene Symbol Accession Synonym

191 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2933331 chr6 + 158164282 158286097 1.06 3173880 chr9 + 70925894 71059931 1.06 3624145 chr15 - 49527223 49702258 1.06 2542816 chr2 - 20291440 20450197 1.06 3662387 chr16 + 55523269 55552122 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 10353 3223738 chr9 - 122699696 122731521 1.06 (continued) 2 // NIP2 2 // 3627076 chr15 - 57742025 57768916 1.06 2 // ZO2 2 MST155 // MST155 // SDP1 MSTP155 // SH3PX1 WISF // SH3PXD3A // INPP5H // // KIAA0348 MGC44422 MGC26306 // X104 X104 // MGC26306 ZO- // FLJ26672 // FLJ26672 RC3 // KIAA0856 FLJ36528 // FLJ36528 // KIAA0235 // MGC138251 // MGC138253 PUMH2 // PUML2 35 // KIAA0025 HERP // SUP Mif1 // 004330 BNIP- 016224 004817 016530 FLJ38125 3597476 chr15 + 61268620 61347018 1.06 015263 005658 MGC: // EBI6 015317 014685 NM_ // NM_ 003898 NM_ // NM_ 201629 40 NM_ // 001010989 NM_ // 001010990 NM_

45 BNIP2 NM_ TJP2 RAB8B NM_ TRAF1 NM_ HERPUD1

50 like domain domain like inducible, associated factor

55 like 2 DMXL2 NM_ sorting nexin 9 // synaptojanin 2 9 // synaptojanin nexin sorting // SYNJ2 SNX9 BCL2/adenovirus E1B 19kDa E1B 19kDa BCL2/adenovirus interacting protein 2 tight junction protein 2 (zona (zona 2 protein junction tight 2) occludens RAB8B, member RAS member RAB8B, family oncogene Dmx- TNF receptor- 1 (Drosophila) 2 homolog pumilio PUM2 NM_ homocysteine- endoplasmic reticulum stress- inducible, ubiquitin- member 1 Gene Name Gene Symbol Accession Synonym

192 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2427074 chr1 - 109742573 109770611 1.06 2322389 chr1 + 16639774 16659570 1.06 2881672 chr5 - 150389707 150446947 1.06 3429312 chr12 + 102848291 102871551 1.06 3703885 chr16 - 86421130 86460615 1.06 3263944 chr10 + 112621575 112649753 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 1 // KIAA0113 KIAA0113 1 // MGC117302 // MGC117302 // MGC125802 // MGC125803 // MGC125B04 ZETA // PSC5 FLJ10420 // RP4- // RP4- FLJ10420 798A10.1 ABIN- // VAN NAF1 // ECGP // GP96 // GP96 // ECGP - TRA1 // // GRP94 // GRP94P1 // HSP // // GRP94b // HSPCP2 // HsGrp94b // TRAP1 TRA1P1 4F2LC // CD98 // // CD98 4F2LC // E16 // D16S469E // // MPE16 LAT1 hLAT1 //DC49 // // MLAS hLAT1-3TM 35 MGC33046 // H731 MGC33047 // 002790 018090 006058 003299 003486 014456 NM_ // NM_ // - 003211 NM_ // NR_ 002593 40 NM_ // NM_ 145341

45 PSMA5 NM_ NECAP2 NM_ HSP90B1 // HSP90B1 // TDG HSP90B2P SLC7A5 // SLC7A5 LAT1-3TM PDCD4

55 proteasome (prosome, (prosome, proteasome type, alpha subunit, macropain) 5 NECAP endocytosis associated 2 TNFAIP3 interacting protein 1 protein interacting TNFAIP3 TNIP1 NM_ heat shock protein 90kDa beta beta 90kDa protein shock heat thymine- 1 // member (Grp94), shock heat // glycosylase DNA (Grp94), beta 90kDa protein 2 (pseudogene) member leupaxin (cationic 7 family carrier solute y+ transporter, acid amino SLC7A5 5 // member system), pseudogene LPXN 004811 NM LDPL 3374402 chr11 - 58050925 58102459 1.06 programmed cell death 4 4 death cell programmed transformation (neoplastic inhibitor) Gene Name Gene Symbol Accession Synonym

193 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3580179 chr14 - 101616842 101676327 1.06 2652410 chr3 + 173240112 173601176 1.06 2498977 chr2 + 108431315 108492470 1.06 Transcript Transcript ID Cluster 2407191 chr1 - 37805043 37834120 1.06 Human ST Exon 1.0

30 1 // (continued) FLJ31884 // HSP86 // HSP86 FLJ31884 // HSP90A // HSPC1 // HSP90N HSPCA // // // HSPCAL1 // HSPN HSPCAL4 // // Hsp90 Hsp89 // // LAP2 // HSP90ALPHA // HSPCAL3 HSP90Af DKFZp686D14170 DKFZp686D14170 // DKFZp762K137 // // FAD104 // FLJ23399 // MGC10002 // PRO4979 YVTM2421 GCC185 // GCC185 // KIAA0336 // hRad50RAD50-2 2828564 chr5 + 131774479 132009928 1.06 FLJ40906 // FLJ40906 // HUMAUANTIG // Ngp- NGP1 35 dJ423B22.6 005348 022763 014635 005732 013285 NM_ // 001017963 NM_ // NM_ // 001040141 - 40 NM_ 181453 // NM NM_ // NM_ 133462

45 SOS2 006939 NM - // HSP90AA1 // HSP90AA2 HSP90AA6P 3563734 chr14 - 49654812 49768331 1.06 FNDC3B NM_ GCC2 GNL2 NM_

50 coil domain domain coil

55 like 2 (nucleolar) 2 like son of sevenless homolog 2 2 homolog of sevenless son (Drosophila) alpha 90kDa protein shock heat 1 // member A class (cytosolic), alpha 90kDa protein shock heat 2 // member A class (cytosolic), alpha 90kDa protein shock heat 6 A member class (cytosolic), (pseudogene) RAD50 homolog (S. cerevisiae) (S. homolog RAD50 RAD50 domain III type fibronectin 3B containing guanine nucleotide binding binding nucleotide guanine protein- GRIP and coiled- and GRIP containing 2 containing Gene Name Gene Symbol Accession Synonym

194 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3542847 chr14 + 70857592 71468470 1.06 3770743 chr17 - 70805871 70913384 1.06 3806211 chr18 - 41817502 41906221 1.06 3536663 chr14 +3527514 chr14 54588114 + 54606655 1.06 20007398 20015985 1.06 2610359 chr3 + 10181579 10260427 1.06 2340529 chr1 + 66030487 66612844 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 2 // 2 // DKFZp686G1344 // DKFZp686G1344 // KIAA0440 E6TP1 ASH // ASH EGFRBP- // // Grb3-3 GRB2 // MST084 MSTP084 MAYP // // MAYP MGC34175 MGC23138 // MISS // MISS MGC23138 // c14 5346 // MGC117396 // MGC125915 PNP // MGC125916 // PRO1837 // PUNP IRAK- MGC150550 35 // DKFZp686F2182 // DPDE4 // MGC126529 PDEIVB 015556 002086 024430 144578 000270 001570 002600 NM_ // NM_ 203506 40 NM_ // 001037339 NM_ // 001037340 NM_ // 001037341 NM_

45 SIPA1L1 NM_ GRB2 PSTPIP2 NM_ C14orf32 NM_ IRAK2 NM_ PDE4B

50 bound bound threonine 1 receptor- 55 serine- induced proliferation- induced signal- associated 1 like1 growth factor receptor- factor growth 2 protein nucleoside phosphorylasenucleoside NPproline- NM_ phosphatase interacting protein protein interacting phosphatase 2 chromosome 14 open reading frame 32 associated kinase 2 interleukin- phosphodiesterase 4B, cAMP- 4B, phosphodiesterase specific (phosphodiesterase E4 (phosphodiesterase specific Drosophila) homolog, dunce Gene Name Gene Symbol Accession Synonym

195 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3301914 chr10 - 98342808 98470259 1.06 2431112 chr1 -2400518 chr1 120205744 120426930 - 1.06 21394307 21544720 1.06 Transcript Transcript ID Cluster 2771654 chr4 -3434413 68020183 chr12 68093837 + 1.06 119456489 119500226 1.06 2555490 chr2 - 61558490 61619343 1.06 Human ST Exon 1.0

30 4 (continued) C // CENPC BETA // BCAP // RP11- // RP11- BCAP 34E5.3 AGS2 // hN2 // // // hN2 AGS2 // DJ328E19.C1.1 // NBPF FLJ35032 // // FE65L ECE // FE65L1 MGC35575 CENP- // hcp- MIF2 // ARG // ABLL // KIAA0262 2446047 // MGC126758 // MGC126764 chr1 - 177335093 177528267 1.06 35 CRM1 // // DKFZp686B1823 ERBA- // GRTH // ERBA2 // MGC126109 // MGC126110 THR1 // // NR1A2 THR82 THR81 // 021813 - 2964553 chr6 - 90692975 91063182 1.06 152309 001397 001812 005158 014868 003400 024408 024408 XM_ // 001133349 NP_ // NM_ 015383 NM_ // NM_ 173075 NM_ 007314 // NM 40 NM_ // NM_ 000461

45 BACH2 NM_ PIK3AP1 NM_ NOTCH2 // NOTCH2 NBPF14 APBB2 // ECE1 ABL2 XPO1 // THRB XPO1

50 a) kinase kinase 3- like) erb-

55 gene) related binding, family B, abl Abelson murine leukemia leukemia murine Abelson abl BTB and CNC homology 1, 1, CNC homology and BTB 2 factor zipper leucine basic endothelin converting enzyme 1 enzyme converting endothelin precursor (A4) beta amyloid // protein- 2 (Fe65- member phosphoinositide- adaptor protein 1 protein adaptor v- 2 (arg, homolog oncogene viral Abelson- 10 protein finger ring // 2 (Drosophila) homolog Notch breakpoint neuroblastoma RNF10 14 member family, NM_ exportin 1 (CRM1 homolog, homolog, 1 (CRM1 exportin hormone thyroid // yeast) (erythroblastic beta receptor, (v- viral leukemia C protein 1centromere CENPC1 NM_ Gene Name Gene Symbol Accession Synonym oncogene homolog 2, avian) 2, homolog oncogene

196 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3740479 chur17 - 1500681 1534906 1.06 2883609 chr5 - 157145339 157284818 1.06 3257098 chr10 + 907215192773023 90765521 chr4 1.06 - 74158547 74343428 1.06 3221916 chr9 - 116138238 116200584 1.06 3088544 chr8 + 20098984 20143098 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0 1 // 30 (continued) 16 HPRP8 // PRP8 // // PRP8 HPRP8 PRPC8 // RP13 CLINT // ENTH // // CLINT // EPNR // EPN4 // EPSINR KIAA0171 ALPS1A // APO- ALPS1A // CD95 // APT1 // FASTM // FAS1 TNFRSF6 // GTAR FLJ22206 // NY- KIAA0697 // BR- KIAA1968 // RP11- // RP11- KIAA1968 8211.4 35 // ATP6B1B2 // // HO57 ATP6B2 VPP3 // // VATB Vma2 006445 014666 000043 152872 152874 152876 032217 015028 2 AD 030767 2705266 chr3 - 172258898 172660964 1.06 001693

40 NM_ // NM_ // 152871 NM_ // NM_ // 152873 NM_ // NM_ // 152875 NM_ // NM_ 152877 NM_ // NM_ 198889

45 PRPF8 NM_ FAS TNIK NM_ ATP6V1B2 NM_

50 mRNA processing 55 hook transcriptionfactor AKNA NM_ PRP8 pre- cerevisiae) (S. homolog 8 factor ankyrin repeat domain 17 domain repeat ankyrin ANKRD17 1 interactor clathrin CLINT1 NM_ Fas (TNF receptor superfamily, superfamily, receptor (TNF Fas 6) member AT- TRAF2 and NCK interacting interacting NCK and TRAF2 kinase transcription ATPase, H+ H+ ATPase, transcription lysosomal transporting, B2 V1 subunit 56/58kDa, Gene Name Gene Symbol Accession Synonym

197 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3456732 chr12 - 53075332 53099491 1.06 3331730 chr11 + 58101868 58149782 1.06 3975467 chrX + 44590716 44896185 1.06 Transcript Transcript ID Cluster 2875555 chr5 - 132238768 132327205 1.06 Human ST Exon 1.0

30 (continued) Rel 2484358 chr2 + 60962266 61004124 1.06 CD49e // FNRA // // FNRA CD49e VLA5A FKSG11 // PZF // PZF // FKSG11 HCNTF // ZNF757 PMCA1 3464983 chr12 - 88505965 88620030 1.06 DKFZp686A03225 DKFZp686A03225 // MGC141941 // // bA386N14.2 DKFZp686L12190 // UTY1 UV20 3865378 chr19 - 50602433 50673926 1.06 35 // // MCEF AF5Q31 MGC75036 002205 153341 FLJ90005 2405312 chr1 - 33172120 33203343 1.06 053023 005239 - 3921068 chr21 + 39059147 39118744 1.06 021140 182659 001983 002908 C- 014423 NM_ // NM_ NM // 170768 000614 NM_ // 001001323 001682 NM NM_ // NM_ // 007125 NM_ // NM_ 182660 40 NM_ // NM_ 202001

45 ITGA5 NM_ ZFP91 // CNTF ZFP91 ETS2 NM_ ATP2B1 UTX // UTY UTX ERCC1 REL NM_

50 linked

55 ets erythroblastosis virus E26 rel reticuloendotheliosis viral viral reticuloendotheliosis rel IBR domain containing 3 IBRDC3 NM_ integrin, alpha 5 (fibronectin 5 (fibronectin alpha integrin, polypeptide) alpha receptor, zinc finger protein 91 homolog homolog 91 protein finger zinc neurotrophic // ciliary (mouse) factor v- (avian) 2 homolog oncogene ATPase, Ca++ transporting, transporting, Ca++ ATPase, 1 membrane plasma ubiquitously transcribed transcribed ubiquitously X repeat, tetratricopeptide chromosome // ubiquitously transcribed tetratricopeptide Y- gene, repeat excision repair cross- repair rodent complementing complementation deficiency, overlapping 1 (includes group sequence) antisense v- (avian) homolog oncogene AF4/FMR2 family, member 4 member family, AF4/FMR2 AFF4 NM_ Gene Name Gene Symbol Accession Synonym

198 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3140213 chr82879509 - chr5 72843959 - 73059105 1.06 143463451 143565514 1.06 2558150 chr2 - 69538639 69783824 1.06 2555630 chr2 - 61939693 61970469 1.06 3740367 chr172530713 - chr2 1423948 + 1478920 228386802 1.06 228427090 1.06 4005644 chrX - 40392502 40480045 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 5 // SMAP5 // SMAP5 // 5 1 // ABF1 // ABF1 1 // 3a // MIP3A // // MIP3A // 3a ABF- MYOR // DKFZp313L2216 // SB140 // FinGER5 SMAP- YIP1A KIAA1048 // // KIAA1048 MGC138170 Cctd // MGC126164 // MGC126164 Cctd // MGC126165 // SRB CAP2 // PI8 // CAP2 3791996 chr18 + 59787618 59823238 1.06 FLJ23848 // LAT4 // LAT4 // FLJ23848 MGC34680 LARC // // CKb4 MIP- // SCYA20 35 // CSRP CRSP150 // CXorf4 // EXLM1 // DRIP150 // MED14 // // MGC104513 // TRAP170 RGR1 005098 030799 014911 006430 002640 152346 004591 004229 NM_ // 001024947 NM_ NM_ // 001031848 NM_ // NM_ 198833 40 XM_ // 001126052 NM_

45 MSC NM_ CCT4 NM_ SERPINB8 SLC43A2 NM_ CRSP2

50 cell C motif) ligand 20 ligand motif) C CCL20 NM_

55 1) Yip1 domain family, member 5 member family, domain Yip1 YIPF5 musculin (activated B- (activated musculin factor- AP2 associated kinase 1 kinase associated AP2 AAK1 NM_ chaperonin containing TCP1, TCP1, containing chaperonin 4 (delta) subunit chemokine (C- chemokine clade inhibitor, peptidase serpin 8 member B (ovalbumin), aryl hydrocarbon receptor hydrocarbon aryl member 43, family carrier solute 2 AHR NM 001621 - 2991233 chr7 + 17304771 17363729 1.06 cofactor required for Sp1 activation, transcriptional 2, 150kDa subunit Gene Name Gene Symbol Accession Synonym

199 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2461786 chr1 -2593464 chr23135184 233396677 chr8 233558145 - 1.06 - 197512324 197901798 1.06 53641628 53789545 1.06 3974838 chrX3143970 + chr8 41055591 - 41108668 1.06 91014745 91066433 1.06 3017547 chr7 + 104436029 104542698 1.06 3139035 chr8 - 68250009 68418446 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 V2 // V2 (continued) V1 // AT- V1 // BCAA // BRCAA1 // BRCAA1 // // BCAA // DKFZp313M2420 // MGC163290 // RBBP1L1 // SAP180 RBP1L1 KIAA0117 // // MGC21968 MGC70444 DRAGOU14OCI // FIP200 // DBX // DDX14 // // DDX14 DBX // HLP2 DDX3 AT- // // FLJ10155 ATV // NBS MGC87362 FLJ10078 // FLJ10078 // FLJ14026 // HDCMC04P MGC70452 ARFGEP1 // BIG1 // // BIG1 // ARFGEP1 // D730028018Rik // DKFZP434L057 P200 35 GTT1 2565143 chr2 - 96214334 96238296 1.06 016374 015014 153697 014781 001356 002485 018682 006421 020151 NM_ // NM_ // 031371 NM_ XM_ // 001129278 NM_ NM- // 001024688 NM_ NM_ // NM_ 182931 40 NM_ // NM_ 139267

45 ARID4B // ARID4B RBM34 DDX3X MLL5 ARFGEF1 NM_

50 coil 1 RB1CC1 NM_ Asp) box box Asp) linked Ala- Glu- inhibited) exchange factor 1 factor exchange

55 or mixed- lymphoid like) // RNA binding motif motif binding RNA // like) ribosylation factor guanine guanine factor ribosylation inducible coiled- inducible ankyrin repeat domain 44 domain repeat ankyrin RB1- ANKRD44 12 peptidase specific ubiquitin NM_ USP12 182488 NM USP12L1 3506738 chr13 26518485 26644264 1.06 nibrin4B domain interactive rich AT (RBP1- 34 protein NBN DEAD (Asp- polypeptide 3, X- 3, polypeptide lineage leukemia 5 (trithorax (trithorax 5 leukemia lineage Drosophila) homolog, myeloid/ (brefeldin A- (brefeldin START domain containing 7 containing domain START STARD7 ADP- nucleotide- Gene Name Gene Symbol Accession Synonym

200 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2939034 chr6 - 2832402 2858242 1.06 2977265 chr6 - 143065515 143308841 1.06 2522616 chr2 + 201689135 201744701 1.06 2421925 chr1 - 89343675 89496682 1.06 3952637 chr22 - 17696576 17799452 1.06 Transcript Transcript ID Cluster 3327906 char11 + 43290109 43322649 1.06 Human ST Exon 1.0 1 2 // 30 FLIPL // FLIPL FLICE // FLICE (continued) 3 // CAP3 // 3 // 11 // AAC11 // // // AAC11 11 EP2 // MBP- CAP- CAP // // P19 DKFZp686104222 // MGC111370 // // // P16 MSTP057 PTI HIV- MIBP1 CASH // // CASP8AP1 // Casper // CLARP // FLAME- FLAME I- // FLIP // // USURPIN MRIT // c- // FLIP c- FLJ38822 // GBP4L GBP4L // FLJ38822 Mpa2 - // // DGCR1 // TUP1 // TUP1 // DGCR1 TUPLE1 35 AAC- AP15L1 002463 MXB 3922037 chr21 + 41655820 41703177 1.06 004155 006734 003879 207398 052941 003325 006595 NM_ // NM_ 004568 40 NM_ // NM_ // 004120 NM_

45 MX2 NM_ SERPINB9 // // SERPINB9 SERPINB6 HIVEP2 NM_ CFLAR NM_ GBP7 // GBP2 // GBP2 GBP7 GBP4 // HIRA NM_

50 like like inducible // guanylate // guanylate inducible 55 myxovirus (influenza virus) virus) (influenza myxovirus 2 (mouse) resistance serpin peptidase inhibitor, clade clade inhibitor, peptidase serpin // 9 member B (ovaibumin), clade inhibitor, peptidase serpin 6 member B (ovalbumin), human immunodeficiency virus virus immunodeficiency human 2 protein binding I enhancer type CASP8 and FADD- and CASP8 regulator apoptosis guanylate binding protein 7 // 7 protein binding guanylate 2, protein binding guanylate interferon- binding protein 4 protein binding HIR histone cell cycle regulation (S. A homolog defective cerevisiae) apoptosis inhibitor 5 inhibitor apoptosis API5 NM_ Gene Name Gene Symbol Accession Synonym

201 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2969886 chr6 - 112088237 112301348 1.06 2779823 chr4 - 103393022 103486067 1.06 3560711 chr14 - 34291692 34414604 1.06 3445670 chr12 - 14829481 14848171 1.06 3090006 chr8 + 23439117 23485313 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) MGC45350 // SLK // SLK // MGC45350 SYN BIGM 103 // LZT- LZT- // 103 BIGM Hs6 ACF1 // // ACF1 // DKFZP586E0518 // WALp1 FLJ14383 // WCRF180 // hACF1 DKFZp779M1063 // DKFZp779M1063 SIPP1 // NPWBP 35 // // MFRN HT015 // MSCP // MSC // PR01278 // PR01584 PR02217 002227// JAK1B JAK1A 2416522 chr1 - 65071504 65278035 1.06 012081 2867873 chr5 - 95246561 95323733 1.06 002037 153048 022154 013448 020980SSC1 // HsT17287 3595594 chr15 + 56217766 56280468 1.06 016312 016612 NM_ // NM_ // 153047 NM_ NM_ // NM_ 182648 40 XM_ // 001128238 XM_ // 001128248 XM_ // 001128255 XM_ // 001128269 NM_

45 JAK1 NM_ ELL2 NM_ FYN SLC39A8 NM_ BAZIA SLC25A37

55 Janus kinase 1 (a protein tyrosine kinase) elongation factor, RNA RNA factor, elongation 2 II, polymerase FYN oncogene related to SRC, SRC, to related oncogene FYN YES FGR, aquaporin 9aquaporin AQP9 NM_ solute carrier family 39 (zinc (zinc 39 family carrier solute transporter), member 8 bromodomain adjacent to zinc 1A domain, finger WW domain binding protein 11 protein binding domain WW WBP11 NM_ solute carrier family 25, member member 25, family carrier solute 37 Gene Name Gene Symbol Accession Synonym

202 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3734865 chr17 + 71022989 71032409 1.06 3680434 chr16 - 11549088 11599620 1.06 2489545 chr2 + 74913290 74974310 1.06 7385547 chr17 + 29513430 29608325 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) CF 1 // MCP1 // 2 //GDCF- 2 REL 3835966 9 chr19 + 50196537 50233287 1.06 FLJ37147 // FLJ37147 // sen54 SEN54L CMT1C // CMT1C // FLJ38636 // MGC116698 // MGC116700 // MGC116701 // MGC125274 // MGC125275 // MGC125276 // // SIMPLE PIG7 TP5317 DKFZp686M1669 // DKFZp686M1669 // HXK2 HKII 35 GDCF- HC11 // HC11 MCAF // HSMCR30 // MCP- SCYA2 // MGC9434 // SMC- 207346 004862 005230SAP2 // // NET ERP 173354 3427098 SIK // MSK chr12 + 3934111 chr21 95112269 95187725 - 1.06 43637578 43705100 1.06 000189 006509 I- 002982

45 TSEN54 NM_ LITAF NM_ ELK3 NM_ RELB NM_

50 cells 3 cells induced induced C motif) ligand 2 ligand C motif) CCL2 NM_ domain protein protein domain

55 like kinase like SNF1LK NM_ rel reticuloendotheliosis viral viral reticuloendotheliosis rel tRNA splicing endonuclease 54 54 endonuclease splicing tRNA (S. cerevisiae) homolog SNF1- lipopolysaccharide- TNF factor ELK3, ETS- ELK3, 2) protein accessory (SRF chemokine (C- chemokine 2hexokinase HK2 NM_ (avian) v- nuclear B, homolog oncogene factorkappa of lightpolypeptide in B- enhancer gene Gene Name Gene Symbol Accession Synonym

203 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3204404 chr9 - 35026106 35062648 1.06 2634494 chr3 + 106304077 106816151 1.06 2496727 chr2 + 101600496 101877880 1.06 3956781 chr22 - 28053592 28206955 1.06 2731381 chr4 +3942179 chr22 74953973 + 74983954 1.06 28609182 28762301 1.06 3906160 chr20 - 39464169 39680547 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0 a // a 30 (continued) DSP1 // DSP1 // 3 // IBMPFD // // MGC131997 // MGC148092 TERA // MGC8560 // FAG // p97 // XRCC9 CD166 // FLJ38514 // CD166 FLJ38514 // MEMD // MGC71733 FLH21957 // FLH21957 // FLJ10410 // FLJ20373 // // HGK FLJ90111 // NIK K1AA0687 ADTB1 // AP105A // // // AP105A ADTB1 CLAPB2 // BAM22 GRO1 GROa // // MGSA // MGSA alpha // MGSA- NAP- FYVE- // KIAA0371 ZFYVE10 35 K1AA1335 // CHD5 // RIGB 007126 001627 004834 145687 001127 001102 FLJ40884 3569814 chr14 - 68409817 68515815 1.06 001511 021090 153051 032221 NM_ // NM_ 004629 NM_ // NM_ // 145686 NM_ NM_ // NM_ 145730 40 NM_ // NM_ // 153050 NM_

45 VCP // FANCG VCP ALCAM NM_ MAP4K4 AP1B1 CXCL1 NM_ CHD6 NM_

50 C motif) ligand ligand motif) C X- activated protein protein activated

55 complex protein related containing protein // protein containing valosin- anemia, Fanconi G group complementation activated leukocyte cell cell leukocyte activated molecule adhesion actinin, alpha 1 alpha actinin, ACTN1 NM_ mitogen- kinase kinase kinase kinase 4 kinase kinase kinase kinase 1, beta 1 subunit 1 beta 1, myotubularinrelated protein 3 MTMR3 adaptor- chemokine (C- chemokine 1 (melanoma growth stimulating stimulating growth 1 (melanoma alpha) activity, chromodomain helicase DNA DNA helicase chromodomain 6 protein binding Gene Name Gene Symbol Accession Synonym

204 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2916716 chr63291682 + chr10 89847048 - 89852045 1.06 64589487 64951821 1.06 2934089 chr6 + 160066607 160097332 1.06 3884450 chr20 + 36095232 36189576 1.06 2510485 chr2 + 151974674 152072768 1.06 3508330 chr13 -2403111 chr1 30558258 30651692 - 1.06 27603331 27689256 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 // 145 (continued) 25 B4-2 // PNAS- B4-2 // PRR2 // PROL2 RP11-63L7.5 // DKFZp761F0118 // FLJ14374 // RP11- KIAAL380 // TRIP8 10C13.2 DKFZp686F20131 DKFZp686F20131 // KLAA0105 // - // MGC3925 CREPT // CREPT // DKFZp434P0735 // FLJ44520 dJ1057B20.2 DKFZp781N1478 // // DKFZp781N1478 FLJ12870 SCAR2 // WAVE2 // // WAVE2 // SCAR2 dJ393P12.2 35 DKFZp686M05240 // HSP105 // // HSP105A // HSP1058 NY- // KIAA0201 CO- 006813 004241 033083 - 2612371 chr3 + 15443374 15466824 1.06 004906 152858 021215 018151 006990 006644 NM_ // NM_ 032776 40 NM_ // NM_ // 152857 NM_ // NM_ 005891

45 PNRC1 NM_ WTAP // // WTAP ACAT2 C20orf77 NM_ RIF1 NM_ HSPH1 NM_

50 110kDa 110kDa

55 rich nuclear receptor receptor nuclear rich jumonji domain containing 1C containing domain jumonji JMJD1C 1 factor associated ELL EAF1 NM_ proline- 1 coactivator Wilms tumor 1 associated associated 1 tumor Wilms A Coenzyme acetyl- // protein 2 (acetoacetyl acetyltransforase thiolase) A Coenzyme chromosome 20 open reading frame 77 WAS protein family, member 2member family, protein WAS WASF2 factor RAP1 interacting (yeast) homolog NM_ heat shock 105kDa/ shock heat 1 protein Gene Name Gene Symbol Accession Synonym

205 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2608765 chr3 + 5138874 5197592 1.06 2749699 chr4 + 160171745 160501468 1.06 3541137 chr143328520 + chr11 66896518 +3131916 66922983 chr8 1.06 44543723 44598484 - 1.06 38251717 38359646 1.06 3319840 chr11 + 9362702 9426296 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 2A // GEP (continued) GEF // Rap // GEF 2 // EIF- 2 // EIF2 2alpha ARL10C // ARL10C // Gie1 FLJ10702 PDZ- // CNrasGEF PDZGEF1 // GEF1 // RA- Rap- GEP // EIF- EIF- EIF2A GR15 // // C33 4F9 // R2 KAI1 // IA4 // // ST6 // // SAR2 // DKFZp667H044 // FLJ20353 // MGC126766 // MGC142029 // pp14328 NSD3 FLJ14581 // FLJ14581 // MGC138673 RANBP7 35 - 2376922 chr1 + 204924896 204974249 1.O6 018184 004094 002231 017778 006391 004759 376350 376350 934717 944403 944412 XM_ // XM_ // 934714 XM_ // XM_ // 934718 XM_ // XM_ // 944410 XM_ NM_ // 001024844 NM_ NM_ // NM_ 023034 40 NM_ // NM_ 032960

45 RAPGEF2 WHSC1L1 EIF2S1 NM_ MAPKAPK2

50 like 8B ARL8B NM_ like 1 like

55 protein activated activated protein kinase kinase protein activated Hirschhorn syndrome syndrome Hirschhorn factor- ribosylation Rap guanine nucleotide nucleotide guanine Rap 2 (GEF) factor exchange CD82 moleculeCD82 Wotf- 1- candidate CD82 ADP- eukaryotic translationinitiation 35kDa 1 alpha, subunit 2, factor importin 7importin 1P07 NM_ kinase- 2 mitogen- Gene Name Gene Symbol Accession Synonym

206 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3154317 chr8 -3553872 chr14 134318628 134379306 + 1.06 103160147 103247456 1.06 2448073 chr1 - 183532162 183553081 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 1 // NS1- BP // BP // NS1- // 1 CAP43 // CMT4D // CMT4D // // CAP43 // // GC4 DRG1 NDR1HMSNL // // // PROXY1 NMSL // // // RTP RIT42 // TDD5 TARG1 KLC // KLC1 // // KNS2A MGC15245 - // FLJ23757- 2560254 chr2 - 74607294 74610455 1.06 35 DKFZp686K06216 // FLARA3 // // FLJ10069 // FLJ10411 // FLJ10962 // FLJ35593 // FLJ36593 // HSPC068 KIAA0850 // ND1 // NS- NS1BP 006096 005552 181575 006469 053064 - 3535628 chr14 + 51383702 51506715 1.06 NM_ // NM_ 182923 NM_ // NM_ 133637 40 NM_ // NM_ 016389

45 TINF2 012461 NM NDRG1 TIN2 NM_ 3558012 chr14 - 23776465 23781950 1.06 AUP1 //DQX1 IVNS1ABP GNG2 NM_

55 myc downstream regulated regulated downstream myc kinesin 2kinesin KNS2 TERF1 (TRF1)-interacting (TRF1)-interacting TERF1 2 factor nuclear N- 1 gene ancient ubiquitous protein 1 // 1 // protein ubiquitous ancient 1 (RNA- polypeptide box DEAQ ATPase) dependent influenza virus NS1A binding binding NS1A virus influenza protein guanine nucleotide binding binding nucleotide guanine 2 gamma protein), (G protein Gene Name Gene Symbol Accession Synonym

207 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3552729 chr14 + 101296771 101464066 1.06 2320727 chr1 + 12149647 12192323 1.06 3647632 chr16 + 9092682 9121055 1.06 3598662 chr15 + 64466253 64571690 1.06 3326635 chr11 + 35117003 35210509 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 I // Pgp1 Pgp1 I // (continued) II // TNF- II // lll // HCELL HCELL // lll R- B56G // MGC23064 // MGC23064 B56G G PR61 // CD120b // TBPII // // // TBPII CD120b TNF- TNFBR // // R75 // TNFR80 // TNFR2 p75 // p75TNFR FLJ41272 // FLJ41272 PRO0149 MAPKK1 // MEK1 // // MEK1 // MAPKK1 // PRKMK1 MKK1 35 // CSPG8 // CDW44 ECMR- // MC56 // LHR IN // // // MDU3 MDU2 // MIC4 // MGC10468 MUTCH- // // FLJ12099 // // // JNK3 FLJ33785 // JNK3A // MGC50974 // PRKM10 p493F12 // 002719 178587 001066 014117 002755 000610 002753 138981 NM_ // NM_ // 178586 NM_ // NM_ 178588 40 NM_ // NM_ // 001001389 NM_ // 001001390 NO_ // 001001391 NM_ // 001001392 NM_ // NM_ // 138980 NM_ // NM_ 138982

45 PPP2R5C TNFRSF1B NM_ C16orf72 NM_ MAP2K1 NM_ CD44 // // CD44 MAPK10

50 ’, gamma activated activated

55 protein activated isoform protein phosphatase 2, phosphatase protein B subunit regulatory tumor necrosis factor receptor receptor factor necrosis tumor 1B member superfamily, chromosome 16 open reading frame 72 kinase kinase 1 kinase kinase mitogen- protein kinase 10 kinase protein CD44 molecule (Indian blood blood (Indian molecule CD44 // mitogen- group) Gene Name Gene Symbol Accession Synonym

208 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2487549 chr23309629 + chr10 - 69995330 70023575 121291481 1.06 121346521 1.06 3489212 chr13 + 48428770 48681909 1.06 2522439 chr2 + 201384456 201418386 1.06 3848689 chr19 - 7929463 7999655 1.06 Transcript Transcript ID Cluster 3978169 chrX + 53124038 53134445 1.06 Human ST Exon 1.0

30 (continued) MAD // MAD1 // MAD1 // MAD MGC104659 TCBP // MGC33401 TIAR // FLJ31509 // FNDC3 // KIAA0970 // // bA203116.1 // bA203I16.5 // RP13- CT45-3 BZAP45 // BZAP45 // KIAA0005 NbIa10236 ELAV1 // HUR // // ELAV1 // MelG // Hua DKFZp686H05241 TIM44 // 35 // // CINAP CDA1 DENTT // // CTCL // HRIHFB2216 // - SE20-4 002357 003252 014923 014670 001419 004760 DRAK1 2999485 chr7 + 43573961 43642649 1.06 022117 NM_ // 001033925 NM_ NM_ // 001079673 NM_ // NM_ 001017435 XM_ // 001126385 NM_ NM_ // NM_ 006351 40 XM_ // 001128695 NM_ // NM_ 000940

45 TIAL1 FNDC3A // FNDC3A RP13-36C9.3 BZW1 ELAVL1 // ELAVL1 TIMM44 TSPYL2 // TSPYL2 PON3 testis

55 like 1 threonine kinase 17a kinase threonine STK17A NM_ like 2 // paraoxonase3 TIA1 cytotoxic granule- cytotoxic TIA1 associated RNA binding binding RNA associated protein- MAX dimerization protein 1 protein dimerization MAX MXD1 NM_ fibronectin type III domain domain III type fibronectin cancer/ 3A // containing CT45-3 antigen basic leucine zipper and W2 and zipper leucine basic 1 domains ELAV (embryonic lethal, lethal, (embryonic ELAV vision, abnormal antigen (Hu 1 Drosophila)-like inner of translocase // R) mitochondrial membrane 44 (yeast) homolog TSPY- serine/ Gene Name Gene Symbol Accession Synonym

209 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3689922 chr16 -2562932 chr2 45220566 45280598 - 1.06 86857923 86889020 1.06 2518428 chr2 +3819880 chr19 182464815 182516732 + 1.06 9112073 9135082 1.06 3181976 chr9 + 101623410 101669157 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 1 // CS1 // CS1 // 1 DKFZp434E1211 // // DKFZp434E1211 // DKFZp434P1672 // FLJ10752 // FLJ13588 // MEM3 FLJ20388 // MAL // Leu2 CD8 // p32 CS- // DKFZp313O1039 // DKFZp779G0129 // FLJ45996 KRAP // KIAA1927 SPAG13 // // KIAA1588 // DKFZp572C163 // FLJ32813 MGC35232 35 CSMF // CHN // NOR1// MINOR // TEC 001514// TFIIB TF2B 2421753 chr1 - 89090909 89130195 1.06 020933 018206 001768 022136 // NASH1 HACS1 3925473 chr21 - 14779427 14877594 1.06 006981 173199 006751 033160 NM_ NM_ // XM_ // 001125688 NM- NM_ // NM_ 171827 40 NM_ // NM_ // 173198 NM_ // NM_ 173200

45 GTF2B // // GTF2B RP11-82K18.3 ZNF317 // ZNF317 ZNF658 VPS35 NM_ SAMSN1 NM_ NR4A3

55 CD8a moleculeCD8a IIB factor transcription general CD8A zinc finger protein 317 // zinc zinc // 317 protein finger zinc 658 protein finger 35 sorting protein vacuolar (S. cerevisiae) homolog sperm specific antigen 2antigen specific sperm SSFA2 NM- SAM domain, SH3 domain and and domain SH3 domain, SAM 1 signals localization nuclear nuclear receptor subfamily 4, 4, subfamily receptor nuclear 3 A, member group Gene Name Gene Symbol Accession Synonym

210 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2982076 chr6 - 159375488 159517834 1.06 2784027 chr4 - 122695163 122838353 1.06 3539070 chr14 + 61225495 61285222 1.06 3227159 chr93289235 chr10 - - 131689314 131845274 51706090 1.06 52054733 1.06 2445141 *2445141 chr1 - 174150358 174443232 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 1alpha // HIF1- // 1alpha - // HB15BL11 2895841 2558511 chr6 chr2 + - 14118209 70290081 14485106 70329315 1.06 1.06 FKSG15 // // FKSG15 // FLJ32631 // FLJ39771 // MGC133247 // MGC27381 TAGAP1 ANX5 // ENX2 // // ANX5 PP4 HIF- MOP1 // // ALPHA PASD8 FBP17 // KlAA0554 KlAA0554 // FBP17 MGC126804 // MOB // MGC17342 // SMS1 MOB1 // 35 // FLJ10416 COP1 RNF200 // 022037 003859 MPDS // CDGIE 3909395 chr20 - 48984632 49008494 1.06 054114 152133 001154 001530 015033 147156 022457 NM_ // NM_ 022173 NM_ // 001040280 004233 NM NM_ // NM_ // 138810 NM_ NM_ // NM_ 181054 40 NM_ // 001001740 NM_

45 TIA1 DPM1 NM_ TAGAP HIF1A RFWD2 loop-

50 inducible factor 1, factor inducible

55 phosphate cell activation GTPase GTPase activation cell CD83 moleculeCD83 CD83 associated RNA binding protein binding RNA associated TIA1 cytotoxic granule- cytotoxic TIA1 dolichyl- mannosyltransferase subunit catalytic 1, polypeptide T- protein activating annexin A5annexin ANXA5 NM_ transmembrane protein 23 protein transmembrane hypoxia- TMEM23 helix- (basic subunit alpha NM_ helix transcription factor) transcription helix formin binding protein 1 FNBP1 NM_ ring finger and WD repeat repeat WD and finger ring 2 domain Gene Name Gene Symbol Accession Synonym

211 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2539821 chr2 - 9546070 9630637 1.06 3976299 chrX + 47300826 47316249 1.06 2773958 chr4 - 77151393 77163693 1.06 2352228 chr1 + 112945824 113015736 1.06 3714729 chr17 + 21128581 21159113 1.06 3645253 chr16 + 2742650 2761908 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 10 // 10 (continued) 1 10 // 10 SCYB10 // KD // 2 // gIP- // 2 RAF // ARAF1 // // // ARAF1 RAF CD156b // CD156b TACE // MGC71942 cSVP // A- RAFA1 // PKS2 C7 // IFI10INP10 // // IP- crg- mob- CAPPA1 // CAPZ // CAPZ // // CAPPA1 CAZI MAPKK3 // MEK3 // // MEK3 // MAPKK3 // PRKMK3 MKK3 35 300- DKFZp686O15166 // FLJ21926 // // FLJ22250 // KIAA0324 // MGC40295 SRm300 // SRL300 003183 001654 001565 021970 MP1 144726 DKFZp686M11215 006135 2884216 chr5 2779408 chr4 - - 158516997 158569129 1.06 101018538 101034726 1.06 145110 016333

40 XM_ // 001130488 NM_ // NM_ NM // 002756 145109

45 ADAM17 NM_ ARAF NM_ CXCL10 NM_ MAP2K1IP1 NM_ CAPZA1 NM_ MAP2K3 SRRM2 NM_

50 C motif) ligand ligand motif) C X- line, alpha 1 alpha line, activated protein protein activated 55 protein activated arginine repetitive matrix raf murine sarcoma 3611 viral viral 3611 sarcoma raf murine ADAM metallopeptidase metallopeptidase ADAM necrosis (tumor 17 domain converting alpha, factor, enzyme) v- homolog oncogene chemokine (C- chemokine 10 hypothetical protein FLJ31951protein hypothetical FLJ31951 filament) (actin protein capping Z- muscle NM_ kinase kinase 1 interacting 1 interacting kinase kinase 1 protein mitogen- kinase kinase 3 kinase kinase mitogen- serine/ 2 Gene Name Gene Symbol Accession Synonym

212 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2692060 chr3 -3376235 chr11 123729469 123766193 - 1.06 62356627 62365857 1.06 2911903 chr6 + 64289625 64351448 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 1 // (continued) - // MGC52424- 3623320 chr15// OA3 // MER6 IAP - 2687739 chr3 47055671 47126043 - 1.06 109143203 109306052 1.06 BAL // BAL1 // BAL1 // BAL // DKFZp666B0810 DKFZp686M15238 // FLJ26637 // // MGC: FLJ41418 7868 // FLJ10439 FLJ21730 35 // DKFZp779M0721 PRL- // HH72 PTP // PRL1 // (CAAX1) PTPCAAX1 014701 174894 001777 031458 018093 003463 NM_ // NM_ // 001042461 NM_ 001042462// NM_ NM_ // 001025079 NM_ // NM_ 198793 40 XM_ // 001125771 NM_

45 KIAA0256 // // KIAA0256 TRAPPC5 PARP9 NM_ PTP4A1 NM_

50 ribose) polymerase polymerase ribose) 55 CD47 moleculeCD47 CD47 WD repeat domain 74 domain repeat WD // product gene KLAA0256 WDR74 particle protein trafficking complex 5 poly (ADP- poly 9 member family, protein tyrosine phosphatase phosphatase tyrosine protein 1 IVA, member type Gene Name Gene Symbol Accession Synonym

213 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3270270 chr10 + 129595315 129774152 1.06 3751625 chr173462949 - chr12 24977091 -3526831 25281397 chr13 1.06 75269250 - 754777203989721 1.06 chrX 113765177 113916197 1.06 + 122922013 123384079 1.06 2532699 chr2 + 233632835 233823600 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0 2 // 2 // 30 (continued) EPSILON 145 // hp51CN // 145 DKFZp313F1310 // // DKFZp313F1310 R- // PTPE // HPTPE PTP- KIAA1725 // // KIAA1725 SSH- // MGC78588 2 DKFZp686A11164 // MGC126578 // // MGC133203 // OSBP10 ORP8 // GAP1IP4BP // GAPIII // MGC46517 // DKFZp686P168 // DKFZp781H1753 // SA- FLJ25871 bA517O1.1 // SA2 35 // MGC104855 // MGC142140 // MGC142142 // // SHIP1 SHIP SIP- 006504 033389 020841 007368 006603 005541 929960 929960 NM_ // NM_ 130435 NM_ // 001003712 NM_ NM_ // 001042749 NM_ // 001042750 NM_ // 001042751 NM_ 40 XM_ // NM_ // 001017915 NM_

45 NEK7PTPRE 133494 NM - 2373736 chr1 + 196225008 196558827 1.06 SSH2 NM_ INPP5D like 8 like OSBPL8

50 5-

55 oxysterol binding proteinbinding oxysterol 3 activator protein RAS p21 RASA3stromal antigen 2 NM_ gene mitosis in (never NIMA 7 kinase a)-related STAG2 phosphatase, tyrosine protein receptortype, E slingshot homolog 2 homolog slingshot (Drosophila) inositol polyphosphate- phosphatase, 145kDa phosphatase, Gene Name Gene Symbol Accession Synonym

214 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3606304 chr15 + 83681343 84102785 1.06 4009315 chrX -3147591 chr8 53575796 53740871 - 1.06 103907725 103953967 1.06 3744680 chr17 - 8718740 8809747 1.06 3884191 chr20 + 35406502 35467847 1.06 3892812 chr20 + 60744242 60787582 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0 3 // 3 // 30 Src (continued) LB // LB // c- LBC 2 // P101- P101- 2 // E // OATP1 // OATP1 E // Lbc // BRX // BRX // // Lbc BP1 // BP1 // AKAP- // FLJ11952 // HA- FLJ43341 // LBC // Ht31 PROTO- PROTO- Ibc ARF- // HECTH9 // 1b772 HSPC272 // KIAA0312 // // MULE // LASU1 // // ESA UREB1 PON // - // MGC3832 // OAZI // MGC691 // OAZIN F730038115Rik // F730038115Rik FOAP- PI3K ASV // SRC1 // c- // c- // SRC1 ASV // p60- SRC 35 OATP- // OATP4A1 // POAT OATPRP1 SLC21A12 // 006738 144767 031407 000940 015878 014308 005417 016354 NM_ // NM_ // 007200 Nm_ NM_ // NM_ // 000446 NM_ NM_ // NM_ 148174 40 NM_ // NM_ 198291

45 AKAP13 HUWE1 // // HUWE1 // PON3 PON1 PIK3R5 NM_ SRC SLCO4A1 NM_

50 Ruppin kinase, kinase, 3-

55 2) viral oncogene homolog homolog oncogene viral 2) src sarcoma (Schmidt- sarcoma src antizyme inhibitor 1 inhibitor antizyme protein (PRKA) anchor A kinase 1 AZIN 13 HECT, UBA and WWE domain domain WWE HECT, UBA and // 1 paraoxonase // 1 containing 3 paraoxonase phosphoinositide- regulatory subunit 5, p101 5, subunit regulatory A- (avian) v- solute carrier organic anion anion organic carrier solute transporter family, member 4A1 Gene Name Gene Symbol Accession Synonym

215 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3511698 chr13 - 42309603 42464520 1.06 3715703 chr17 + 24013260 24053809 1.06 3362719 chr11 - 10487574 10788746 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0 5 30 (continued) 3 // JP3 // // // JP3 3 BRESI1 // // BRESI1 // MGC29634 // CAGL237 // // HDL2 FLJ44707 JP- TNRC22 KIAA0162 // // KIAA0162 SPT6 // MGC87943 // SPT6H // emb- 35 // // DAP5 AAG1 // NAT1 FLJ41344 p97 001 033255 032482 // KIAA1814 DOT1 3816264 chr19 + 2114945 2183576 1.06 152313// PAT4 FLJ38932 3386638 chr11 - 92485640 92570746 1.06 003170 001418 NM_ // 002264 NM_ // NM_ 020655 40 NM_ // 001042559 NM_

45 EPSTI1 // JPH3 EPSTI1 DOT1 LDOT1 NM_ SLC36A4 NM_ SUPT6H NM_ EIF4G2

55 like, histone H3 epithelial stromal interaction 1 interaction stromal epithelial 3 junctophilin // (breast) DOT1- (S. methyltransferase cerevisiae) amino acid symporter), member member symporter), acid amino 4 solute carrier family 36 (proton/ 36 family carrier solute suppressor of Ty 6 homolog (S. homolog 6 Ty of suppressor cerevisiae) eukaryotic translationinitiation factor 4 gamma, 2 Gene Name Gene Symbol Accession Synonym

216 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 4017381 chrX -3336422 chr11 106803586 106916423 + 1.06 66161951 66190547 1.06 3166718 chr9 + 33015173 33029946 1.06 Transcript Transcript ID Cluster 3601387 chr15 + 72073603 72126162 1.06 Human ST Exon 1.0

30 2 (continued) 22R // 22R hDIP 2 // DjA1 // HDJ2 HDJ2 // // DjA1 2 DIP // DIP // DKFZp313A1123 GILZ // // DSIPI TSC- DKFZp547K0918 // // DKFZp547K0918 MGC75138 // LARK // RBM4A // // ZCCHC21 ZCRB3A DJ- // // HSJ2 HSDJ // hDJ- // HSPF4 35 // // PP8675 MYL TRIM19 // RNF71 004089 002896 001539 002675 033239 033244 033247 033250 NM NM // 001015881 NM_ // NM_ 198057 40 XM_ // 001132060 NM_ // NM_ // 033238 NM_ // NM_ // 033240 NM_ // NM_ // 033246 NM_ // NM_ // 033249 NM_

45 TSC22D3 DNAJA1 NM_

55 RNA binding motif protein 4 RBM4 NM_ TSC22 domain family, member member family, domain TSC22 3 promyelocytic leukemia PML DnaJ (Hsp40) homolog, 1 A, member subfamily Gene Name Gene Symbol Accession Synonym

217 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3356115 chr11 + 129444931 129519895 1.06 3932148 chr21 - 39479279 39615332 1.06 2478748 chr2 + 42250017 42418636 1.06 2763805 chr4 - 24128159 24250940 1.06 3346584 chr1 + 101722704 101754720 1.06 2371255 chr1 + 181708036 181834004 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0 7

30 (continued) 2 // MIHB // MIHB 2 // APPH // APPL2 // // // APPL2 APPH CDEBP C21orf107 // C21orf107 // // N143 FLJ43918 WDR9 C2orf2 // C2orf2 DKFZp686P18118 // ELP120 // // FLJ10942 // FLJ32318 ROPP120 DBP1 // DDX15 // // DDX15 // DBP1 // // PRP43 HRH2 // PrPp43p PRPF43 AP11 // HIAP2 // HIAP2 // AP11 Hiap- cIAP1 RNF48 // 35 // EST1C // C1orf16 // FLJ23717 // KLAA0250 // SMG- SGA56M 001642 018963 002721 - 3225348 chr9 - 126948675 126991992 1.06 019063 001358 001166 014837 201568 NM_ // 001007246 NM_ // NM_ 033656

40 NM_ // NM_ // 173156 NM_ // NM_ 201569

45 APLP2 NM_ BRWD1 PPP6C NM_ EML4 NM_ DHX15 NM_ BIRC2 NM_ SMG7 like

50 His) box box His) Ala- Glu-

55 7 homolog, nonsense nonsense 7 homolog, amyloid beta (A4) precursor- beta (A4) amyloid 2 protein bromodomain andWD repeat 1 containing domain protein phosphatase 6, catalytic catalytic 6, phosphatase protein subunit echinoderm microtubule microtubule echinoderm associated protein like 4 DEAH (Asp- polypeptide 15 polypeptide baculoviral IAP repeat- IAP baculoviral containing 2 containing Smug- factor decay mRNA mediated (C. elegans) Gene Name Gene Symbol Accession Synonym

218 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2436132 chr1 - 151900372 151910103 1.06 2645764 chr3 + 143077611 143128338 1.06 2874794 chr5 - 130760272 131160628 1.06 Transcript Transcript ID Cluster 3762519 chr17 - 46394554 46553215 1.06 Human ST Exon 1.0 1 3870824 chr19 - 59557066 59578582 1.06 30 (continued) 3 // CD298 // // // CD298 3 2 // MGC8391 // NF45 // // NF45 MGC8391 PRO3063 CD305 // LAIR- CD305 ATPB- FLJ29027 DKFZp667N084 // // DKFZp667N084 DKFZp686115116 LB // K1A001 // // GEF2 PDZ- RA- // PDZGEF2 GEF- DKFZp686E18167 P0215 DKFZp781 // // KIAA1961 // MGC667 35 // FLJ13450 // FLJ14006 // // HLC4 FLJ34602 // // JLP HSS // KIAA0516 // MGC117291 // MGC14967 PHET // MGC74461 // PIG6 004515 002287 001679 016340 133372 003971 NM_ 021706 // NM XM_ // 001133533 XM_ // 001133534 NM_ NM_ // NM_ // 001008738 NM_ 40 NM_ // NM_ 172345

45 ILF2 NM_ LAIR1 ATP1B3 RAPGEF6 // RAPGEF6 FNIP1

50 like receptor 1 receptor like associated associated 55 Interleukin enhancer binding binding enhancer Interleukin 45kDa 2. factor leukocyte- immunoglobulin- ATPase, Na+/K+ transporting, transporting, Na+/K+ ATPase, 3 polypeptide beta sperm associated antigen 9 antigen associated sperm SPAG9 nucleotide guanine Rap 6 // (GEF) factor exchange 1 protein interacting folliculin Gene Name Gene Symbol Accession Synonym

219 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3331487 chr11 + 57235839 57391291 1.06 3181193 chr9 + 99202471 99298225 1.06 3452231 chr12 - 44863120 44952390 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 31 // // 31 CGI- // DKFZp781O2021 // MGC111151 // TMX2 // PIG26 // CTNND CAS // KIAA0384 // P120CAS // p120 P120CTN DKFZp761N202 3717635 chr17 + 27701159 27759429 1.06 KIAA1529 // // KIAA1529 // PCTAIRE2BP // RP11-508D10.1 TRAP 35 // NAT2 // ATA1 SNAT1 // SAT1 001 001 015959 001331 003457 021943// TEX27 FLJ13222 2905664 chr6 + 37895285 38231400 1.06 014290 030674 NM_ // XM_ // 126721 XM_ // 001126756 XM_ // 001126767 XM_ // 001126781 XM_ // 001128793 XM_ // 001126823 NM_ NM_ // 001032293 NM_ 40 NM_ // 001077484 NM_

45 TXNDC14 // CTNND1 SLC38A1

50 type domain 3 domain type ZFAND3 NM_

55 zinc finger protein 207 protein finger zinc AN1- finger, zinc ZNF207 thioredoxin domain containing containing domain thioredoxin (cadherin- catenin // 14 associated protein), delta 1 delta protein), associated tudor domain containingtudor 7 TDRD7 NM_ solute carrier family 38, member member 38, family carrier solute 1 Gene Name Gene Symbol Accession Synonym

220 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2911303 chr6 + 57062631 57143064 1.06 3712041 chr17 + 16223047 16228977 1.06 3469687 chr12 - 105155796 105222139 1.06 2618940 chr3 + 412113562668351 41256934 chr3 1.06 - 33404835 33456874 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 // 1a (continued) 63 // // 63 63 // 1B // LBP- COASTER // // FLJ90693 // KIAA0576 // MGC26701 dJ417I1.1 FLJ25987 // FLJ25987 // MGC8385 // FLJ25777 MGC40157 CLIMP- ERGIC- // p63 MGC99554 DKFZp686L1745 // // DKFZp686L1745 LBP- 35 // CTNNB FLJ25606 // LBP1A 015555 030627 KIAA1673 2841699 chr5 + 173177911 173320580 1.06 020453 // ATPVD 2726072 chr4 + 47179942 47290260 1.06 018955 006825 014517 001904 005337 HEM1 3416577 chr12 + 53177769 53224156 1.06 NM_ // 001031623 NM_ NM_ // NM_ 152350 40 XM_ // 001133660 XM_ // 001133664 XM_ // 001133673 XM_ // 001133675 NM_

45 ZNF451 // ZNF451 KIAA1702 CPEB4 NM_ UBB // UBB C17orf45 CKAP4 NM_ UBP1 NM_ CTNNB1 like NCKAP1L NM_ 50 associated associated associated protein protein associated

55 1a) associated protein 1- zinc finger protein 451 protein finger zinc cytoplasmic polyadenylation polyadenylation cytoplasmic 4 protein binding element ATPase, Class V, type 10D V, type Class ATPase, ATP10D NM_ ubiquitin B // chromosome 17 17 // chromosome B ubiquitin 45 frame reading open 4 NCK- cytoskeleton- upstream binding protein 1 protein binding upstream (LBP- catenin (cadherin- catenin 88kDa 1, beta protein), Gene Name Gene Symbol Accession Synonym

221 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3800619 chr18 - 16783710 17017478 1.06 2658346 chr3 + 194793673 194902403 1.06 2982319 chr6 - 160020086 160103541 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) B // MNSOD // // MNSOD B SOD MGC131603 // MGC131603 // MGC43611 P160ROCK FLJ12460 // FLJ12460 // // NPG KIAA0567 // largeG NTG 35 IPO- Mn- 005406 015560 30832 // 130833 130835 130837 000636 NM_ // NM_ // 130831 NM_ NM_ // NM_ // 130834 NM_ // NM_ // 130836 NM_ 40 NM_ // NM_ // 001024465 NM_ 001024466

45 ROCK1 NM_ OPA1 SOD2 // SOD2 MGC5618

50 coil

55 associated, coiled- associated, Rho- 1 kinase protein containing optic atrophy 1 (autosomal (autosomal 1 atrophy optic dominant) superoxide dismutase 2, dismutase superoxide mitochondrial Gene Name Gene Symbol Accession Synonym

222 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2491615 chr23233547 chr10 + + 85597809 85625908 6170982 1.06 6225410 1.06 3754677 chr17 - 32949033 33043613 1.06 2603051 chr2 - 230740259 230797812 1.06 3922100 chr21 + 41714183 41752955 1.06 Transcript Transcript ID Cluster 3891163 chr20 + 56848165 56919604 1.06 Human ST Exon 1.0

30 (continued) 43 2320048 chr1 + 10995025 11013170 1.06 78K // IFI78 // IFI78 // 78K MATA2 // MATII // // MATII MATA2 SAMS2 // MGC14439 SPF45 MGC104959 // MGC104959 SYNG FLJ22835 // IF141 // // IF141 FLJ22835 VODI // IF175 IFI- MxA // MX 35 // C20orf45 // AHO // GPSA GNAS1 GSP // GSA // // MGC33735 PHP1B // // PHP1A POH // // dJ309F20.1.1 dJ806M20.3.3 005911 032905 007247 007375 TDP- 004509 080424 002462 000516 016592 080426 NM_ // NM_ 080550 NM_ // NM_ // 004510 NM_ 40 NM_ // NM_ // 001077488 NM_ // 001077489 NM_ // 001077490 NM_ // NM_ // 080425 NM_ // NR_ 003259

45 MAT2A NM_ AP1GBP1 SP110 MX1 NM_

50 inducible protein p78 protein inducible 55 RNA binding motif protein 17 RBM17 NM_ TAR DNA bindingTAR DNA proteinmethionine alpha II, adenosyltransferase TARDBP NM_ AP1 gamma subunit binding binding subunit gamma AP1 1 protein interferon- (mouse) SP110 nuclear body body SP110 nuclear (mouse) protein GNAS complex locus GNAS virus) (influenza myxovirus 1, resistance Gene Name Gene Symbol Accession Synonym

223 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3431483 chr123167325 + chr9 109203332 + 109352495 1.06 34168995 34243205 1.06 3595096 chr15 + 54963208 55402126 1.06 3776193 chr18 + 2688138 2794997 1.06 3766960 chr173159483 - chr9 59968891 + 60088896 460301 1.06 746375 1.06 3809671 chr18 - 53418770 53448841 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) ATP2B // DAR // DD ATP2B // MGC45367 // SERCA2 // MGC119669 NAG20 // MGC8710 UAP // // HEB // HTF4 // // HTF4 HEB HsT17266 DKFZp68600631 // // DKFZp68600631 KIAA0650 DKFZp686F0270 // // DKFZp686F0270 MGC138150 // G231 DKFZp451 // KIAA0172 KANK MGC43128 // 35 // ASNRS SFX3 // BA108L7.2 001681 016525 003205 207037 207040 022739 015158 175854 - 3483159 chr13 + 27572646 27773671 1.06 004539 113962 113962 NM_ // NM_ 170665 NM_ // NM_ // 207036 NM_ // NM_ // 207038 NM_ XM_ // XM_ 938891 NM_ // NM_ 153186 40 NM_ // NM_ 030971

45 ATP2A2 TCF12 SMCHD1 SMURF2 NM_ PAN3 NM_ NARS // SFXN3

50 tRNA synthetase // tRNA synthetase helix transcription transcription helix 55 loop- ubiquitin associated protein 1protein associated ubiquitin UBAP1 NM_ ATPase, Ca++ transporting, transporting, Ca++ ATPase, cardiac muscle, slow twitch 2 transcription factor 12 (HTF4, (HTF4, 12 factor transcription helix- 4) factors ankyrin repeat domain 15 domain repeat ankyrin of maintenance structural ANKRD15 hinge flexible chromosomes 1 containing domain SMAD specific E3 ubiquitin ubiquitin E3 specific SMAD 2 ligase protein PAN3 polyA specific specific polyA PAN3 homolog subunit ribonuclease cerevisiae) (S. asparaginyl- 3 sideroflexin Gene Name Gene Symbol Accession Synonym

224 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3240987 chr10 + 30762872 30791283 1.06 3421897 chr12 + 68901823 69035035 1.06 3711262 chr173824713 + chr192880932 + 14145125 chr5 14193444 17972961 1.06 - 17985905 1.06 148800168 148922811 1.06 Transcript Transcript ID Cluster Human ST Exon 1.0

30 COT (continued) 2 // c- 2 // MEKK2 // MEKK2BMEKK2 2574798 chr2 - 127772731 127863022 1.06 COT // EST // ESTF // EST // COT TPL2 // FLJ10486 // TpI- // CDC36 // HSPC131 // CDC36 NOT2 // 35 30ST3B1 // 3OST3B1 // CLONE24945 PP2703 HLCDGP1 // // CK1 PRO2975 014999 KIAA0118 3422269 chr12 + 70434927 70470787 1.06 174907 MGC131930 003286 TOPI 2629693 chr3 + 3885464 chr20 73019946 + 73201035 1.06 39090891 39186535 1.06 003470// TEF1 HAUSP 3679564 chr16 - 8893458 8964832 1.06 006609 005204 014515 006041 015683 001892 XM_ // 001128799 NM_ 40 NM_ // 001025604 NM_ NM_ // 001025105 NM_

45 RAB21 NM_ PPP4R2 NM_ USP7 NM_ MAP3K2 MAP3K8 NM_ CNOT2 NM_ HS3ST3B1 NM_

50 associated) activated protein protein activated 55 protein activated NOT transcription transcription NOT sulfotransferase 3B1 sulfotransferase O- topoisomerase (DNA) Itopoisomerase 7 peptidase specific ubiquitin virus- (herpes TOP1 NM_ RAB21, member RAS member RAB21, family oncogene protein phosphatase 4, phosphatase protein 2 subunit regulatory kinase kinase kinase 2 kinase kinase kinase mitogen- kinase kinase kinase 8 kinase kinase kinase mitogen- arrestindomain containing 2 ARRDC2 11, alpha kinase casein CCR4- CSNK1A1 2 subunit complex, heparan sulfate (glucosamine) (glucosamine) sulfate heparan 3- Gene Name Gene Symbol Accession Synonym

225 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3974708 chrX + 40829542 40980776 1.05 2694644 chr3 - 130369369 130385467 1.05 2777333 chr4 - 89401891 89424935 1.06 2402111 chr1 - 25440667 25538017 1.06 Transcript Transcript ID Cluster 3263624 chr10 + 111944059 112037108 1.06 Human ST Exon 1.0

30 (continued) DFFRX // FAF // FAF // // DFFRX AZFA // // AZF SP3 // DFFRY CNBP1 // DM2 // // DM2 CNBP1 RNF163 // PROMM ZCCHC22 // ZNF9 // DKFZp667B084 // DKFZp667B084 // DKFZp761G058 // PTMP UG0882E07 DJ465N24.2.1 // DJ465N24.2.1 // RP3- NPD014 465N24.4 35 // MAD2 // MGC43220 MXD2// MXI 004654 003418 002647 // MGC61518 3786039 chr18 + 37534028 37985705 1.05 152542 005124 HNUP153 // N153 2943808 chr6 - 17723255 17855638 1.06 020317 000104 GLC3A B // CP1 2548699 chr2 - 38138730 38196009 1.06 005966 - 2520225 chr2 + 191205069 191437200 1.06 005962 NM_ // 001039590 NM_ // 001039591 NM_

40 NM_ // 001008541 NM_ // NM_ 130439

45 USP9X // USP9X USP9Y CNBP NM_ PIK3C3 NM_ PPM1K NM_ C1orf63 NM_ CYP1B1 NM_ NAB1 NM_

50 kinase, kinase, 3- linked (fat facets- (fat linked

55 type zinc finger, nucleic nucleic finger, zinc type A binding A protein(EGR1 1 ubiquitin specific peptidase 9, X- 9, peptidase specific ubiquitin specific // ubiquitin linked 9, Y- peptidase Drosophila) like, CCHC- protein binding acid phosphoinositide- class 3 protein phosphatase 1K (PP2C 1K phosphatase protein containing) domain nucleoporin 153kDanucleoporin NUP153 NM_ chromosome 1 open reading reading open 1 chromosome frame 63 cytochrome P450, family 1, 1, family P450, cytochrome 1 B, polypeptide subfamily MAX interactor 1 interactor MAX NGFI- protein binding MX1 Gene Name Gene Symbol Accession Synonym

226 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3147321 chr8 - 103333634 103493671 1.05 2593670 chr2 - 197962756 198039327 1.05 3006572 chr73282213 + chr103186966 68695979 - chr9 69896399 27439066 1.05 + 27484191 1.05 119506334 119670150 1.05 3759849 chr17 - 40869050 40923923 1.05 3340913 chr11 + 75803897 75941697 1.05 2476219 chr2 + 32435095 32697447 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) DD5 // EDD // // EDD DD5 // // HYD FLJ11310 // KIAA0896 MGC57263 PRP10 // PRPF10 // PRPF10 // PRP10 SF3b155 // SAP155 KIAA0442 // // KIAA0442 MGC13140 // MEG4 // FTSH L YME1 // PAMP // // TOLL CD284 hToll AP162 // B2 // // B2 AP162 KIAA0356 EMSY // FLJ90741 GL002 // 35 // APOLLON // BRUCE // FLJ13726 // FLJ13786 015902 012433 015570 014263 139313 138554 020193 016252 NM_ // 001005526 NM_ NM_ // NM_ // 139312 NM_ 40 XM_ // 001128220 014798 NM

45 EDD1 NM_ SF3B1 AUTS2 NM_ PLEKHM1 C11orf30 NM_ BIRC6 NM_

55 like(S. 1 cerevisiae) YME1 L1 like receptor 4 receptor like TLR4 NM_ E3 ubiquitin protein ligase, ligase, protein ubiquitin E3 HECT domain containing, 1 YME1- toll- 1, subunit 3b, factor splicing 155kDa autism susceptibility candidate candidate susceptibility autism 2 pleckstrin homology domain domain homology pleckstrin containing, family M (with RUN 1 member domain) chromosome 11 open reading frame 30 baculoviral IAP repeat- IAP baculoviral containing 6 (apollon) containing Gene Name Gene Symbol Accession Synonym

227 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2463864 chr1 - 241354364 241485236 1.05 3096428 chr8 + 43030413 43060080 1.05 3649890 chr16 + 15950935 16144419 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) X // MRP // MRP // X // FAM68A // KAB // // FAM68A // KIAA0470 // FAM68B // KIAA0470L MGC26143 FPTA // MGC99680 // MGC99680 FPTA // PGGT1A 35 ABCC // // ABC29 DKFZp686N04233 DKFZp781G125 // // GS- MRP1 014812 002027 004996 019898 019900 019902 002664// P47 FLJ27168 2486811 chr2 + 68415853 68526386 1.05 017916 017916 XM_ // 001125768 NM_ // 001042404 NM_ // 001042405 NM_ // XR_ // 015931 XR_ // NR_ 003135 NM_ // 001018676 NM_ // 001018677 NM_ 40 NM_ // NM_ // 019862 NM_ // NM_ // 019899 NM_ // NM_ // 019901 NM_

45 CEP170 // CEP170 CEP170L FNTA ABCC1

55 binding cassette,sub- centrosomal protein 170kDa // 170kDa protein centrosomal 170kDa- protein centrosomal like pleckstrin PLEK NM_ farnesyltransferase, CAAX box, CAAX box, farnesyltransferase, alpha ATP- family C (CFTR/MRP), member member (CFTR/MRP), C family 1 Gene Name Gene Symbol Accession Synonym

228 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2879312 chr5 - 142566614 142794517 1.05 3822049 chr193753500 + chr17 - 12910423 12916480 30696595 1.05 30724798 1.05 3717737 chr17 + 27795087 27834449 1.05 2998536 chr7 + 39897668 40103253 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 1 // ILF1 1 // 3738969 chr17 + 78070883 78195807 1.05 (continued) GCCR//GCR// GR // GCCR//GCR// GRL FLJ26680 // RO // // RO FLJ26680 // cC1qR SSA // FLJ34922 SLFN8/9 MGC3844 // S9 // S9 // // MGC3844 p44.5 CDC2L CDC2L // CHED // // FLJ35215 KIAA1791 35 ILF // ILF- 000176 004343 152270 002815 003718 182557 // DLNB11 BCL9-2 3393993 chr11 - 118272076 118304947 1.05 004514 NM_ // NM_ // 001018074 NM_ // 001018075 NM_ // 001018076 NM_ // 001018077 NM_ // 001020825 NM_ 001024094 NM_ // NM_ 031267 40 XM_ // 001134363 XM_ // 001134364 NM_

45 NR3C1 PSMD11 NM_ CDC2L5

50 like BCL9L NM_ like 5 related cell cell related iyvnphoma 9- iyvnphoma 55 cell CLL/ schlafen family member 11 member family schlafen SLFN11 NM_ 3, subfamily receptor nuclear 1 member C, group (glucocorticoid receptor) calreticulin CALR NM_ proteasome (prosome, (prosome, proteasome non- subunit, 26S macropain) ATPase, 11 ATPase, cell division cycle 2- cycle division cell (cholinesterase- controller) division forkhead box K2 box forkhead B- FOXK2 Gene Name Gene Symbol Accession Synonym

229 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3958253 chr222674179 - chr3 31113563 - 31138223 1.05 49290730 49353046 1.05 3512948 chr13 - 45814156 45917111 1.05 3035892 chr7 - 2724003 2910140 1.05 3063337 chr7 - 98922007 98935856 1.05 Transcript Transcript ID Cluster 3444958 chr12 - 12510545 12606611 1.05 Human ST Exon 1.0

30 (continued) 7 // MKP7 7 10//LYT10 3261643 chr10 + 104144262 104152716 1.05 DJ149A16.6 // // DJ149A16.6 RP1- HSPC117// 149A16.6 MGC149848// // UNP MGC149849 // Unph LYT- FLJ21562 // FLJ21562 FLJ43762 MGC 104623 // // 104623 MGC NNX3 // MGC99644 // gep RMP // CD42d // FLJ12298 // CD42d FLJ12298 ZKSCAN14 // 35 // KIAA1700 // MGC129701 // MGC129702 MKP- 014306 003363 002502 025113 007353 003017 SRp20 2905118 chr6 + 36669658 36741293 1.05 004488 030640 NM_ // NM_ 199443 NM_ // 001077493 NM_ // 001077494 NM_ 40 NM_ 032164 // NM

45 C22orf28 NM_ USP4 NFKB2 C13orf18 NM_ GNA12 NM_ SFRS3 NM_ NPAT 002519 NM E14 3390067 chr11 - 107533176 107599902 1.05 GP5 // ZNF394 GP5

50 serine-

55 oncogene) ubiquitin specific peptidase 4 4 peptidase specific ubiquitin (proto- chromosome 22 open reading frame 28 nuclear factor of kappa light light of kappa factor nuclear in B- enhancer gene polypeptide cells 2 (p49/p100) chromosome 13 open reading frame 18 guanine nucleotide binding binding nucleotide guanine 12 alpha protein) (G protein rich 3 nuclear protein, ataxia- protein, nuclear telangiectasia locus arginine/ factor, splicing glycoprotein V (platelet) // zinc // zinc (platelet) V glycoprotein 394 protein finger dual specificity phosphatase 16 phosphatase specificity dual DUSP16 NM_ Gene Name Gene Symbol Accession Synonym

230 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3732885 chr17 + 64019700 64059052 1.05 3961842 chr22 - 39969442 40028027 1.05 2502300 chr2 + 118243834 118323562 1.05 2767378 chr4 - 42105160 42353857 1.05 2892738 chr6 + 3966500 4010215 1.05 2552153 chr2 - 47869608 47988296 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) iso // XTP2 iso 2367154 chr1 + 169716078 169829262 1.05 CAR // CNC // CNC1 DKFZp779L0468 // // MGC17251 // PRKAR1 // // PKR1 Fug1 // KIAA1835 // // KIAA1835 // Fug1 // MGC20266 FLJ33908 // MrDb // // // MrDb FLJ33908 - ATPASEII // ATPIA // ATPASEII // ATPP2 // // MGC130042 // MGC130043 // MGC26327 // FLJ20124 // FLJ20383 MGC163154 K1AA0536 // PR4H // PR4H K1AA0536 // // PRP4H PRP4 // // PRP4K dJ1013A10.1 35 FLJ12673 // FBX11 // MGC44383 // // PRMT9 VIT1 // UG063H01 002734 212472 002883 006773 003414 HZF2 3657367 chr16 + 31730255 31836159 1.05 006095 003913 012167 025133 NM_ // NM_ // 212471 NM_ NM_ // NM_ 003393 NM_ // NM_ 017675 40 NM_ // NM_ // 018693 NM_

45 PRKAR1A RANGAP1 NM_ DDX18 // // DDX18 WNT8B ATP8A1 // ATP8A1 PCLKC PRPF4B NM_ type type 50 Asp) box box Asp) Ala- Glu- mRNA processing 55 box protein 11 protein box FBXO11 dependent, regulatory, type I, I, type regulatory, dependent, specific (tissue alpha 1) extinguisher protein kinase, cAMP- kinase, protein Ran GTPase activating protein 1 BAT2 domain containing 1containing domain BAT2 BAT2D1 015172 NM BAT2- zinc finger protein 267 protein finger zinc DEAD (Asp- ZNF267 NM_ polypeptide 18 // wingless- family, site integration MMTV 88 member ATPase, aminophospholipid aminophospholipid ATPase, I, type Class (APLT), transporter // protocadherin 1 member 8A, LKC PRP4 pre- factor 4 homolog(yeast) B F- Gene Name Gene Symbol Accession Synonym

231 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 Transcript Transcript ID Cluster 2745499 chr4 + 144325529 144364549 1.05 2609608 chr3 + 9414309 9495916 1.05 Human ST Exon 1.0

30 (continued)

35 // FLJ35970 // HP43.BKD KIAA1891 DKFZp686J18276 // FLJ10707 // KIAA1757 002468 - 2617563 chr3 + 38155029 38159513 1.05 032557 926615 926615 931417 931447 931478 944260 944280 944298

40 XM_ // XM_ // 931376 XM_ // XM_ // 931444 XM_ // XM_ // 931455 XM_ // XM_ // 939712 XM_ // XM_ // 944276 XM_ // XM_ // 944295 XM_ // XM_ NM // 944303 001080517

45 DRAM 018370 NM FLJ11259 3428783 chr12 + 100795270 100930011 1.05 MYD88 NM_

55 autophagy regulated damage- modulator 5 containing domain SET SETD5 primary differentiation myeloid response gene ubiquitin specific peptidase 38 peptidase specific ubiquitin USP38 NM_ Gene Name Gene Symbol Accession Synonym

232 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2677653 chr3 - 56629203 56692517 1.05 3309215 chr10 - 120621551 120830522 1.05 3200982 chr9 - 20334968 20612522 1.05 3556888 chr14 - 22439714 22458231 1.05 Transcript Transcript ID Cluster 3923436 chr21 + 44256650 44350842 1.05 Human ST Exon 1.0

30 (continued) 1 // EHOC1 // EHOC1 1 p170 // elF3- // p170 DKFZp686C2456 // // DKFZp686C2456 // KIAA1105 // se89-1 RAP140 EIF3 // EIF3A // EIF3A // EIF3 // P167 // KIAA0139 elF3- p185 // p180 // theta AF9 // FLJ2035 // FLJ2035 // AF9 YEATS3 CAPERbeta // CAPERbeta // FLJ10482 PP239 // MGC4468 RNPC4 // // // SR278 FLJ37706 EHOC- 35 // GT334 // MGC126777 015224 003750 004529 018107 020207 003274 NM_ // 001077351 NM_ // 001077352 NM_ // NM_ // 001034155 NM_ 40 NM_ // 001001723 NM_

45 C3orf63 NM_ E1F3S10 NM_ MLLT3 NM_ RBM23 // RBM23 C9orf102

55 or mixed- lymphoid chromosome 3 open reading reading open 3 chromosome frame 63 eukaryotic translationinitiation theta, 10 subunit 3, factor 150/170kDa lineage leukemia (trithorax (trithorax leukemia lineage Drosophila); homology, to, translocated myeloid/ transmembrane protein 1 protein transmembrane TMEM1 RNA binding motif protein 23 // reading open 9 chromosome frame 102 Gene Name Gene Symbol Accession Synonym

233 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 Transcript Transcript ID Cluster 3320169 chr11 + 10428461 10485703 1.05 Human ST Exon 1.0

30 (continued)

35 // // MGC2237 - MGC2452 NRIC1 // // PPAR // hPPAR // // MGC99627 MTO2// MTU1 // // // TRMT1 TRMT B99 // TRNT1 005036 000480 032644 005038 016426

40 NM_ 001025390 NM_ // NM_ // 018006 NM016426 NM_ // NM_ // 001025389 NM_ // 001025390 NM_ // 001001929 NM_ // 001001930 NM_ // NM_ // 001001928 NM_ // NM_ // 018006 NM_

45 AMPD3 // AMPD3 // PPARA TRMU // GTSE1 50 2- phase expressed 1 expressed phase

55 2 and S- 2 and methylaminomethyl- adenosine monophosphate monophosphate adenosine E) // (isoform deaminase proliferator- peroxisome // tRNA alpha receptor activated 5- thiouridylate methyltransferase methyltransferase thiouridylate // G- Gene Name Gene Symbol Accession Synonym

234 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3429566 chr12 + 103374529 103679918 1.05 3708826 chr17 + 7416768 7423040 1.05 3335907 chr11 + 65573499 65593343 1.05 2659577 chr3 + 197951145 198043895 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 1 // 1 30 4A // (continued) C4ST // C4ST- // C4ST // C4ST1 HSA269537 DDX2A // EIF- DDX2A // EIF4A // DKFZP586K0919 // DKFZp762A152 SSP3 // SMT3IP1 - 2446567 chr1 - 179095658 179258656 1.05 SAP145 // SAP145 // // SF3b1 SF3B145 SF3b150 PAK65 // // PAK65 PAKgamma 35 RAR // NR1B1 3720921 chr17 + 35718982 35767411 1.05 018413 015670 001416 005819 005819 006842 002577 NM_ NM_ // NM_ 015670 NM_ NM_ XM_ // 001126110 NM_ 40 NM_ // 001033603 NM_ 001024809 NM_ // 001033603 NM_ // 000O964 NM_ 001024809

45 CHST11 NM_ E1F4A1 // E1F4A1 SENP3 SF3B2 NM_ PAK2

55 syntaxin 6 4) (chondroitin carbohydrate 1t sulfotransferase STX6 eukaryotic translationinitiation factor 4A, isoform 1 // specific SUMO1/sentrin/SMT3 3 peptidase splicing factor 3b, subunit 2, 2, subunit 3b, factor splicing 145kDa retinoic acid receptor, alpha receptor, acid retinoic RARA kinase (CDKNIA)-activated p21 2 Gene Name Gene Symbol Accession Synonym

235 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3543481 chr14 + 72672571 72760151 1.05 3222144 chr9 - 116695445 116732620 1.05 35941293231774 chr10 + + 500987402920475 50146174 chr6 942450 1.05 + 10558622756673 1.05 108987684 chr4 109112650 1.05 - 833110 916149 1.05 2475209 chr2 + 28828128 28879300 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 1B 30 (continued) AD3 // FAD // PS1 // // // PS1 FAD // AD3 S182 CD153 // CD30L // // // CD30L CD153 // CD30LG MGC138144 DKFZp686F03189 DKFZp686F03189 // ERK3 // // HsT17250 PRKM6 // CRFG // FLJ10686 // FLJ10690 // // NGB FLJ39774 // AF6q21 // DKFZp781A0677 FKHRL1 // // FKHRL1P2 // MGC12739 MGC31925 // FLJ40395 MGC99654 MGC3672 // PP- // MGC3672 35 PPP1CD // 000021 001244 002748 012341 012341 001455 005255 206877 002709 NM_ NM_ NM_ // NM_ 201559 XM_ // 001127411 NM_ 40 NM_ // NM_ NM_ 208876 // 206877 NM_ // NM_ 208876

45 PSEN1 NM_ TNFSF8 NM_ MAPK6 NM_ PPP1CB

55 protein activated presenilin 1 (Alzheimer disease disease (Alzheimer 1 presenilin 3) GTP binding protein 4 protein binding GTP GTPBP4 O3A box forkhead 2 protein transmembrane FOXO3A kinase associated G cyclin TMEM2 GAK tumor necrosis factor (ligand) 8 member superfamily, 013390 NM - 3209384 chr9 - 73452177 73573229 1.05 kinase 6 mitogen- protein phosphatase 1, catalytic catalytic 1, phosphatase protein isoform beta subunit, Gene Name Gene Symbol Accession Synonym

236 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2870397 chr5 - 108614328 108773545 1.05 3192525 chr9 + 134535243 134581784 1.05 3765689 chr17 - 57374750 57498031 1.05 3553337 chr14 + 102313566 102447585 1.05 3153428 chr8 - 131133540 131525100 1.05 3335089 chr11 + 64857703 64877276 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 d4 (continued) 1 // CD40bp // // CD40bp 1 // K1AA0438 // K1AA0438 // Neurodap1 RNF131 FLJ21002 // FLJ21002 // MGC138450 // // TFIIIC90 TFIII90 // TFIICdelta TFiiiC2-90 ARC250 // DRIP250 ARC250 // // HSPC221 // // K1AA0593 CAP- LAP1 // CRAF1 AMAP1 // ASAP1 // ASAP1 // // AMAP1 PAG2 // KIAA1249 PAP // // 35 // REQ MGC10180 // ubi- UBID4 // 003171 SUV3 3250204 chr10 + 70609946 70638996 1.05 014819 012204 005121 003300 145726 018482 005066PSF // POMP100 2406064 chr1 - 35351696 35506894 1.05 006268

40 NM_ // NM_ // 145725 NM_

45 SUPV3L1 NM_ PJA2 NM_ GTF3C4 NM_ THRAP1 NM_ TRAF3 DDEF1 NM_ SFPQ NM_ DPF2 NM_

50 like 1 (S. 1 like H2 motif motif H2 associated factor rich (polypyrimidine 55 suppressor of var1, 3- var1, of suppressor cerevisiae) praja 2, RING- praja containing general transcription factor IIIC, IIIC, factor transcription general 90kDa 4, polypeptide thyroid hormone receptor receptor hormone thyroid 1 protein associated TNF receptor- 3 development and differentiation differentiation and development 1 factor enhancing splicing factor proline/ factor splicing glutamine- tractbinding protein associated) D4, zinc and double PHD fingers fingers PHD double and zinc D4, 2 family Gene Name Gene Symbol Accession Synonym

237 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2507495 chr22976113 + chr6 - 136215526 136259081 1.05 137560317 137582279 1.05 2849469 chr5 - 14757920 14924876 1.05 3996404 chrX + 153318480 153324978 1.05 3420713 chr12 + 65946048 65994719 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 4

30 (continued) FLJ23318 // FLJ23318 // KIAA0242 // erasin UBXDC1 // CD119 FLJ45734 IFNGR // // GDIL // FLJ41411 // MRX48 // MRX41 OPHN2 // // RABGD1A RABGDIA // XAP- ANK // CCAL2 // // CCAL2 ANK // CPPDD CMDJ // HANK FLJ27166 // MANK DKFZp434M1414 // DKFZp434M1414 // FLJ10114 // FLJ10929 // FLJ38691 // FLJ90441 // TIP120 KIAA0829 TIP120A // 35 - 2383726 chr1 + 226313262 226353506 1.05 014607 000416 001493 004685 - 3506153 chr13 - 24700317 24774271 1.05 054027 018448 001658 XM_ // 001132013 NM_ 40 NM_ // 001024226 NM_ // 001024227 NM_ // 001024228 M_

45 ANKH CAND1 NM_

50 dissociated 1 dissociated

55 associated and and associated ribosylation factor 1factor ribosylation ARF1 interferon gamma receptor 1 receptor gamma interferon IFNGR1 1 inhibitor dissociation GDP NM_ GDI1 NM_ UBX domain containing 2 containing domain UBX UBXD2 NM_ myotubularinrelated protein 6 MTMR6 NM_ ankylosis, progressive homolog (mouse) cullin- neddylation- ADP- Gene Name Gene Symbol Accession Synonym

238 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3629811 chr15 - 63737458 63871676 1.05 2806799 chr5 + 36894163 37115932 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) B // BCON3 // BCON3 // B // FLJ33949 // IRLB // // // IRLB FLJ33949 // KIAA0476 MYCPBP CDLS // CDLS // DKFZp434L1319 // FLJ11203 // FLJ12597 // FLJ13354 // FLJ13648 // IDN3 // FLJ44854 IDN3- // FLJ27109 // MADM FLJ35541 MUDPNP // NRBP // 35 - 2713555 chr3 - 198863016 198960684 1.05 032390Nopp34 // NIFK 2573786 chr2 - 122132489 122231052 1.05 005848 015384 013392 032901 032901 NM_ // NM_ // 133433 NM_ 40 XM_ // XM_ 936700

45 MKI67IP NM_ DENND4A NM_ NIPBL // // NIPBL NRBP1

55 B homolog (Drosophila) (Drosophila) B homolog MADD domain domain MADD MK167 (FHA domain) nucleolar interacting phosphoprotein DENN/ 4A containing KIAA0226Nipped- binding receptor nuclear // KIAA0226 1 protein Gene Name Gene Symbol Accession Synonym

239 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3452145 chr123320604 - chr11 + 44599187 44672160 11819556 1.05 11937446 1.05 2868904 chr5 - 100116166 100293502 1.05 3080033 chr7 - 151462947 1517639743401704 1.05 chr12 + 4232432 4284764 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 3 // NPI // NPI // // 3 (continued) IV TS2 // TS2 CASP11 // SIP1 // SIP1 // CASP11 SRRP129 DKFZp686C13257 // FLJ20727 // MGC34450 // MGC34450 // PST MGC61459 // SIAT8D // PST1 ST8SIA- DKFZp686C08112 DKFZp686C08112 // FLJ12625 // // // HALR FLJ38309 // KIAA1506 // MGC119851 // MGC119852 // MGC119B53 ADAM- 35 ADAMTS- // II PCPNI PCINP // hPCPNI // FLJ23119 // FLJ27465 RIPK6 // KIAA1790 // - Roco1 // // KIAK0002 MGC102758 004719 005668 001206BTEB1 // BTEB 3208995 chr9 - 72189344 72219360 1.05 004508 IPPI1 // IPP1 3273601 chr10 - 1075869 1092634 1.05 021230 014244 024652 001759 017944 NM_ // NM_ 175052 40 NM_ // NM_ // 170606 NM_ // NM_ // 021599 NM_ // NM_ 182481

45 SFRS2IP NM_ ST8SIA4 MID11 NM_ MLL3 // // ADAMTS2 // LRRK1 BAGE3 serine-

50 2,8- acetyl- diphosphate delta delta diphosphate N- richrepeat kinase 1 // like factor 9 factor like KLF9 NM_ 55 or mixed- lymphoid ubiquitin specific peptidase 47 peptidase specific ubiquitin USP47 M_ Kruppel- splicing factor, arginine/ factor, splicing rich2, interacting protein ST8 alpha- ST8 neuraminide alpha- neuraminide sialyltransferase 4 sialyltransferase cyclin D2isopentenyl- CCND2 NM_ isomerase 1 isomerase lineage leukemia 3 // ADAM // ADAM 3 leukemia lineage with metallopeptidase 2 motif, 1 type thrombospondin // leucine- myeloid/ family, antigen B melanoma member 3 Gene Name Gene Symbol Accession Synonym

240 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2831932 chr5 + 140006890 140022229 1.05 2897172 chr6 + 18385558 18650038 1.05 2436754 chr1 -3307939 152821187 chr10 152867095 1.05 - 116180867 116571234 1.05 3445786 chr12 - 14986174 15005951 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 4 // 4 (continued) GDI // CSA2 // IK protein // // IK protein CSA2 // RED MGC59741 KIAA0161 // // KIAA0161 // MGC71786 // bA528A10.3 p53RFP ADAR1 // DRADA // DRADA // // ADAR1 // DSRAD DSH 1FI- // G1P1 // K88dsRBP IFI4// p136 // ABLIM // DKFZp781D0148 // FLJ14564 // KIAA0059 // LIMATIN LIMAB1 MGC1224 // 35 // // GDIA2 D4 // // LYGDI GDID4 Ly- 006083 182757 001111 015841 002313 004660 DBY 4030162 chrY + 13525423 13555808 1.05 018119 // SIN RPC5 3652489 chr16 + 22216140 22253905 1.05 001175 000527 // FHC FH 3821015 chr19 + 11061114 11115050 1.05

40 NM_ // 001025107 NM_ // NM_ // 015840 NM_ NM_ // 001003407 NM_ // 001003408 NM_ // NM_ 006720

45 IK NM_ ADAR DDX3Y NM_ POLR3E NM_ ARHGDIB NM_ LDLR NM_

50 Asp) box box Asp) regulator of regulator linked Ala- Glu-

55 IK cytokine, down- IK cytokine, HLA II actin binding UM protein 1protein UM binding actin ABLIM1 IBR domain containing 2 IBRDC2 NM_ adenosine deaminase, MRNA- deaminase, adenosine specific DEAD (Asp- polypeptide 3, Y- 3, polypeptide polymerase (RNA) III (DNA (RNA) III polymerase E (80kD) polypeptide directed) Rho GDP dissociation inhibitor inhibitor dissociation GDP Rho (GDI) beta low density lipoprotein receptor receptor lipoprotein density low (familial hypercholesterolemia) Gene Name Gene Symbol Accession Synonym

241 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2878662 chr5 - 140874773 140978866 1.05 3415229 chr12 + 50717248 50739539 1.05 3614087 chr15 - 23006655 23355108 1.05 2655688 chr3 +3322775 chr11 185514970 185535829 + 1.05 18372531 18386528 1.05 Transcript Transcript ID Cluster 3149843 chr8 - 117909861 117956284 1.05 Human ST Exon 1.0

30 (continued) 1 // NGFIB // NGFIB 1 // M // LDH1 // // LDH1 M DFNA1 // DRF1 // DRF1 // // DFNA1 // LFHL1 FLJ25265 hDIA1 // GFRP1 // HMR GFRP1 // N10 // MGC9485 NAK- // NUR77 // NP10 TR3 ANCR // AS // E6- AS // // ANCR // // EPVE6AP AP // FLJ26981 HPVE6A DKFZp686A1451 // // DKFZp686A1451 // // EIF4G EIF4F p220 LDH- PIG19 35 // FLJ25655 // // HR21 FLJ40596 // HRAD21 // MCD1 KIAA0078 // SCC1 NXP1 // hHR21 005219 002135 173158 000462 130839 004953 198241 198244 005566 006265 NM_ // 001079812 NM_ NM_ // NM_ // 173157 NM_ NM_ // NM_ // 130838 NM_ 40 NM_ // NM_ // 182917 NM_ // NM_ // 198242 NM_

45 DIAPH1 NR4A1 UBE3A EIF4G1

55 diaphanous homolog 1 homolog diaphanous (Drosophila) nuclear receptor subfamily 4, 4, subfamily receptor nuclear 1 A, member group associated protein, Angelman Angelman protein, associated syndrome) lactate dehydrogenase A dehydrogenase lactate E3A ligase protein ubiquitin E6- virus papilloma (human LDHA NM_ eukaryotic translationinitiation factor 4 gamma, 1 RAD21 homologRAD21 (S. pombe) RAD21 NM_ Gene Name Gene Symbol Accession Synonym

242 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3135452 chr8 - 54790669 54918651 1.05 2382117 chr12788195 + chr43690597 - 221955990 chr16 222031806 1.05 - 146274170 146471942 1.05 47130140 47324384 1.05 3075566 chr7 - 138378808 138445046 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 11 // MSTP042 // MSTP042 11 CGI- SFDalpha SFD // // // SFDbeta // VMA13 CANPL2 // CANPml // CANPL2 // FLJ39928 // // DKFZp434I0721 // HSHIN1 // HIN1 KIAA1046 // FLJ31821 KIAA0615 KIAA0079 3251848 chr10 + 75174138 75210008 1.05 35 // DKFZp686F2052 // DKFZp686H1869 DKFZp686019171 // FL86421 // // FLJ13288 // ZAP // MGC48898 // ZC3H2 ZC3HDC2 015941 213620 004566 PFK2 // IPFK2 3233605 chr10 + 6226893 6336597 1.05 001748 017493 153029 004922 020119 NM_ // NM_ // 213619 NM_ NM_ // NM_ 199324 NM_ // NM_ 198597 40 NM_ // NM_ 024625

45 ATP6V1H PFKFB3 NM_ SEC24C ZC3HAV1 50 kinase/ type, antiviral antiviral type, 2- biphosphatase 3 biphosphatase

55 2,8- phosphofructo- ATPase, H+ transporting, transporting, H+ ATPase, V1 subunit 50/57kDa, lysosomal H OTU domain containing 4 containing domain OTU OTUD4 1 protein binding Nedd4 6- N4BP1 NM_ fructose- calpain 2, (m/ll) large subunitlarge (m/ll) 2, calpain CAPN2 NM_ SEC24 related gene family, family, gene related SEC24 C (S. cerevisiae) member 1 zinc finger CCCH- Gene Name Gene Symbol Accession Synonym

243 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3257204 chr10 + 91059126 91090705 1.05 3377226 chr11 - 64376790 64404202 1.05 3599280 chr15 + 65898917 66277975 1.05 Transcript Transcript ID Cluster 3375648 chr11 - 61488337 61492603 1.05 Human ST Exon 1.0

30 (continued) II // II 49 // GARG- 49 49 G - 3502497 chr13 + 112905835 112967356 1.05 FLJ42622 // FLJ42622 // H- FLJ44618 HPAST1 // // PAST PAST1 // PAST CIG- // IFIT4 // IFI60 // // // ISG60 IRG2 RIG- DDXBP1 // GBP // // DDXBP1 GU/RH- // 878 MGC141 // MGC141879 ZMIZ3 35 // // FTHL6 // FTH - // MGC104426 // PLIF // P1G15 FTHL5 003589 003975 TSAd // F2771 2438575 chr1 005475 LNK 014547 - UTMOD 155038957 155053637 3431892 3594066 1.05 chr12 chr15 + + 110328135 49909087 110373802 50026784 1.05 1.05 006795 001549 016166 002202 002202 002201 002204 NM_ // 001008895 NM_ NM_ // 001031683 NM_ 40 NR_ // NM_ // 002032 NR_ NR_ // - // 002205 NR_ // NR_ 002203

45 IFIT3 PIAS1 NM_ FTHL7 // FTH1 // FTHL7 // FTHL3 // FTHP1 // // FTHL12 // FTHL11 FTHL8 like 8 like 7 like 3 50 like 11 // like 12 // ferritin, // ferritin, 12 like induced protein with with protein induced 55 domain containing 1 containing domain EHD1 NM_ cullin 4Acullin 2A protein domain SH2 SH2D2A CUL4A NM_ EH- (ubiquitous) 3 tropomodulin TMOD3 NM_ SH2B adaptor protein 3 protein adaptor SH2B SH2B3 NM_ interferon- tetratricopeptide repeats 3 repeats tetratricopeptide // ferritin, heavy polypeptide 1 // 1 // polypeptide heavy // ferritin, polypeptide- heavy ferritin, polypeptide heavy ferritin, // heavy // ferritin, 1 pseudogene polypeptide- ferritin, heavy polypeptide- heavy ferritin, polypeptide- heavy polypeptide- heavy ferritin, activated of inhibitor protein 1 STAT, Gene Name Gene Symbol Accession Synonym

244 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3261544 chr10 + 103993260 104132642 1.05 3334025 chr11 +3768015 63362634 chr17 63435067 - 1.05 62485987 62672547 1.05 2945645 chr6 - 24758144 24775240 1.05 3739679 chr17 - 375959 564837 1.05 Transcript Transcript ID Cluster 3598959 chr15 + 65145043 65296818 1.05 Human ST Exon 1.0

30 (continued) 1 FLJ21263 // FLJ21263 // FLJ21500 // KIAA0248 // MGC134877 134878 MGC EMK1 // MGC99619 // MGC99619 EMK1 PAR- // DRHC // HUMORF5 MGC // KIAA0054 // 163454 AD022 // EAP2 // // EAP2 AD022 // MGC111021 // MGC9099 dJ30M3.3 FLJ10979 // FLJ10979 // MGC39512 // hVps53L 35 // DKFZP586N0721 DKFZp686J10186 // HSPC193 // JV15- // HsT17436 // MADH3 // 2 // Smad MGC60396 3 004193 004954 014877 016614 018289 005902

40 NM_ // 001039468 NM_ // 001039469 NM_ // NM_ 017490

45 GBF1 NM_ MARK2 TTRAP NM_ VPS53 NM_ 50

55 specific brefeldin A brefeldin specific microtubule affinity- microtubule helicase with zinc finger zinc with helicase HELZgolgi- 1 factor resistance NM_ regulating kinase 2 kinase regulating MAP/ TRAF and TNF receptor receptor TNF and TRAF associated protein vacuolar protein sorting 53 53 sorting protein vacuolar (S. cerevisiae) homolog SMAD family member 3 family SMAD SMAD3 NM_ Gene Name Gene Symbol Accession Synonym

245 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3147508 chr8 - 103682306 103767558 1.05 3257850 chr10 + 93548049 93633726 1.05 2512330 chr2 +3412008 160277236 chr12 160333585 1.05 + 40917957 41128677 1.05 3635198 chr15 - 78040295 78138851 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 // 2 (continued) VII // 5b // PARP- 5b // 1 // ACC- 1 DSC92 // NEUGRINDSC92 3607998 chr15 + 88586640 88670084 1.05 EGRA // TIEG // // TIEG // EGRA TIEG1 PARP- // // PARP5B 5c TANK2 // PARP5C TNKL // AXO // AXOT // // AXOT // AXO // DKFZP586F1122 MARCH- RNF177 // HSPC206 // HSPC232 MGC48786 35 ACC- // BFL1 // BCL2L5 HBPA1 GRS // 016845 130446 FLJ00029 2708066 chr3 - 184688052 184789879 1.05 025235 022826 016488 01439 // 201440 004049 015000 NDR2 // KIAA0965 3409081 chr12 + 27288343 27370157 1.05 NM_ // 001033088 NM_ NM_ // 001032282 005655 NM 40 NM_ // NM_ // 201438 NM_ NM_ // NM_ 201515

45 NGRN TNKS2 NM_ MARCH7 NM_

50 ribose ribose interacting interacting associated ring

55 10 factor like KLF10 related ADP- related threonine kinase 38 like STK38L NM_ related protein A1 protein related BCL2A1 NM_ like 6 (Drosophila) 6 like KLHL6 NM_ Kruppel- neugrin, neurite outgrowth outgrowth neurite neugrin, associated kelch- periphilin 1periphilin TRF1- tankyrase, PPHLN1 ankyrin- polymerase 2 polymerase membrane- 7 (C3HC4) finger BCL2- serine/ Gene Name Gene Symbol Accession Synonym

246 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2507209 chr2 + 135392283 135432746 1.05 3454006 chr12 - 48316548 48387433 1.05 3882854 chr20 + 32414702 32562859 1.05 2553911 chr2 -3429460 chr12 55627936 +3548929 55699519 chr14 1.05 103130628 103354079 + 1.05 92049804 92225160 1.05 3766893 chr17 - 59924843 59935796 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 12 // 12 FLJ90560 // FLJ90560 - // MGC134840 DKFZp762B245 // DKFZp762B245 // FLJ45265 FHOD3 // MGC45819 // AIF4 // AIP4 // AIP4 // AIF4 // NAPP1 dJ46801.1 FLFL2 // FLJ31474 // FLJ31474 FLFL2 // PSY2 // KIAA1387 // smkl GRIM- TR // // MGC9145 TRXR1 // // TR1 TXNR // DKFZp782H1813 // FLJ11700 FLJ22439 35 DKFZp686J01190 // // HLR1 G17P1 // HUMP68 // p68 001241 138326 005721 ARP3 2501697 chr2 + 114360575 114502125 1.05 175738 031483 020463 003330 182742 024832 004396 NM_ // NM_ // 058241 NM_ NM_ // NM_ 198900 40 NM_ // NM_ // 182729 NM_ 182743 // NM

45 CCNT2 // CCNT2 ACMSD ACTR3 NM_ ITCH NM_ SMEK2 NM_ DDX5 NM_

50 Asp) box box Asp) Ala- Glu- related protein 3

55 like 3 like FMNL3 cyclin T2 // T2 cyclin aminocarboxymuconate decarboxylase semialdehyde ARP3 actin- (yeast) homolog KIAA0174formin- KIAA0174 014761 NM MGC117220 3667766 chr16 + 70481983 70522196 1.05 thioredoxin reductasethioredoxin 1 TXNRD1 3 interactor Rab and Ras ubiquitin E3 homolog itchy RIN3 (mouse) ligase protein NM_ SMEK homolog 2, suppressor of of suppressor 2, homolog SMEK (Dictyostelium) mek1 DEAD (Asp- polypeptide 5 polypeptide Gene Name Gene Symbol Accession Synonym

247 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3151401 chr8 - 124094605 124123781 1.05 3333711 chr11 + 62380117 62412872 1.05 2932360 chr6 + 155029299 155324283 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 1 // DER1 // // DER1 1 DER- // FLJ13784 // FLJ42092 // MGC3067 PRO2577 // PDE7HCP1 3138464 chr8 - 66789124 67101393 1.05 4F2 // 4F2HC // // 4F2HC 4F2 // CD98 // 4T2HC MDU1 // // CD98HC NACAE 35 // KIAA1116 // STEF FLJ41865 024295 002603 014892 012454 001068top2beta // TOPIIB 2666478 chr3 - 25614141 25681392 1.05 NM_ // NM_ 002604 NM_ // 001012661 NM_ // 001012662 NM_ // 001012663 NM_ // 001012664 NM_ // 001013251 002394 NM 40 NM_ // NM_ // 001010927 NM_

45 DERL1 NM_ SLC3A2 RBM16 // RBM16 TIAM2 TOP2B NM_

55 like domain family, family, domain like cell lymphoma invasion and and invasion lymphoma cell phosphodiesterase 7Aphosphodiesterase PDE7A Der1- member 1 solute carrier family 3 (activators amino neutral and dibasic of 2 member transport), acid RNA binding motif protein 16 // T- metastasis 2 topoisomerase (DNA) II beta beta (DNA) II topoisomerase 180kDa Gene Name Gene Symbol Accession Synonym

248 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3079803 chr7 - 150865031 151205160 1.05 2814527 chr5 + 70699177 70899402 1.05 3460593 chr12 - 64816984 64850064 1.05 3227696 chr9 - 133441988 133605262 1.05 3723378 chr17 + 40654831 40680464 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 119 // S1R // // S1R 119 13 // 13 AAKG // AAKG2 // AAKG2 // // AAKG // // H91620p CMH6 WPWS DKFZp686C01233 DKFZp686C01233 DKFZp688K0831 // // HSA238520 // // KIAA1241 // KIAA1689 // // TFC5 TAF3BI TFIIIB" // TFIIB150 // TFNR TFIIIB90 // CGI- ZPRO C3G // // DKFZp781P1719 GRF2 35 // C17orf1B C17orf1 // FHOD4 // FMNL// KW- // MGC133052 // MGC1894 021252 RAB18LI1 3240095 chr10 + 27791811 27930577 1.05 016203 007067 // HBOA HBO1 014734 025090 3725779 DUB1 chr17 + 3772581 45196447 3542145 chr17 43261455 chr14 1.05 - + 74295075 69145907 74348574 69250533 1.05 1.05 018429 016056 005312 005892 NM_ // 001040633 NM_ 024429 // NM 40 NM_ // NM_ 198679

45 RAB18 NM_ PRKAG2 MYST2 NM_ BDP1 NM_ TMBIM4 NM_ RAPGEF1

50 activated, activated, catalytic subunit catalytic

55 like 1 like FMNL1 NM_ RAB18, member RAS member RAB18, family oncogene KIAA0247 36 peptidase specific ubiquitin USP36 AMP- kinase, protein 2 non- gamma NM_ KIAA0247 NM_ MYST histone histone MYST 2 acetyltransferase B double prime 1, subunit of of 1, subunit prime B double III RNA polymerase IIIB factor initiation transcription transmembrane BAX inhibitor BAX inhibitor transmembrane 4 containing motif Rap guanine nucleotide nucleotide guanine Rap 1 (GEF) factor exchange formin- Gene Name Gene Symbol Accession Synonym

249 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3298738 chr10 - 88184999 88286267 1.05 2862950 chr5 - 74700067 74843717 1.05 2420808 chr1 - 85504067 85516171 1.05 3473083 chr12 - 114868853 115419724 1.05 2437417 chr13374746 - chr11 - 153571685 153798937 1.05 59160770 59193099 1.05 Transcript Transcript ID Cluster 2722377 chr43773532 chr17 + - 26415653 26636427 77091456 1.05 77105797 1.05 3240340 chr10 + 28828043 29005095 1.05 Human ST Exon 1.0

30 E10 // (continued) 016 // // 016 FOE // KIAA0261 // // // KIAA0261 FOE WAPL CERT // CERTL // // CERTL CERT // GPBP FLJ20597 STARD11 // CARMEN // CIPER // c- CLAP // mE10 DKFZp781D0112 // // DKFZp781D0112 // KIAA FLJ21627 1025 //MED13L // // PROSIT240 TRAMP240L ASH1 // ASH1L1 // ASH1L1 // ASH1 // FLJ10504 KIAA1420 // MGC125671 MGC125672 FLJ39527 // KIAA1 // KIAA1 FLJ39527 482 ACT // ACTG // DNA26 DFNA20 // 35 BM- // MGC10753 // //Wwp4 PRO1741 // bA48B24 bA48B24.1 015045 005713 003921 015335 018489 152716 020860 001614 016628 100486 NM_ // NM_ 031361

40 NM_ // NM_ // 100264 NM_

45 WAPAL NM_ COL4A3BP THRAP2 NM_ ASHIL NM_ WAC

50 like homolog homolog like coil lymphoma 10 lymphoma BCL10 NM_ 55 cell CLL/ wings apart- wings (Drosophila) collagen, type IV, alpha 3 alpha IV, type collagen, binding antigen) (Goodpasture protein B- FLJ36874 proteinFLJ36874 receptor hormone thyroid 2 protein associated FLJ36874 NM_ actin, gamma 1 gamma actin, or small, 1 (absent, ash (Drosophila) homeotic)-like ACTG1 NM_ WW domain containing adaptor adaptor containing domain WW coiled- with stromal interaction molecule 2 STIM2 NM_ Gene Name Gene Symbol Accession Synonym

250 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3961496 chr22 - 39136248 39362660 1.05 3685183 chr16 - 23381059 23429320 1.05 3212143 chr9 - 85464717 85512928 1.05 3680610 chr16 - 11865619 11917408 1.05 Transcript Transcript ID Cluster 2881521 chr5 - 150050460 150060885 1.05 3066297 chr7 - 104537547 104842466 1.05 Human ST Exon 1.0

30 (continued) A 1 // DIO1 // // DIO1 1 BSAC // MAL // // // MAL BSAC MRTF- FLJ20966 // FLJ20966 VEAR // KIAA1080 DA41 // DSK2 // DSK2 // // DA41 // PUC- 1 FLJ90054 // XDRP1 // BYE1 // // DATF1 C20orf158 // // DID03 DIDO2 // DIO- // DKFZp434P1115 // FLJ11265 // KIAA0333 // MGC16140 dJ885L7.8 551 G9.2 // ETF3A // ETF3A G9.2 551 // eRF3a GST1 // FLJ10290 // FLJ10290 ZC3H16 35 // FLJ36101 SFRSK2 020831 002827 PTP1B 3888721 chr20 + 48560298 48634700 1.05 006931 // GLUT3 FLJ90380 3442854 chr12 - 7917549 7980138 1.05 015044 013438 022105 080796 001270 DKFZp686E2337 002094 2868523 chr5 - 98218502 98293051 1.05 018047 82691 // 182692 NM_ // NM_ // 053067 NM_ // NM_ // 033081 NM_ // NM_ 080797 40 NM_ NM_

45 MKL1 NM_ PTPN1 NM_ SLC2A3 NM_ GGA2 NM_ UBQLN1 // UBQLN1 DIDO1 CHD1 NM_

55 receptor type 1 type receptor megakaryoblastic leukemia 1 (translocation) protein tyrosine phosphatase, phosphatase, tyrosine protein non- solute carrier family 2 (facilitated (facilitated 2 family carrier solute 3 member transporter), glucose golgi associated, gamma ARF ear containing, adaptin 2 protein binding obliterator 1 obliterator ubiquilin 1 // death inducer- death 1 // ubiquilin G1 to S phase transition 1 transition S phase to G1 GSPT1 NM_ chromodomain helicase DNA DNA helicase chromodomain 1 protein binding SFRS protein kinase 2kinase protein SFRS RNA binding motif protein 22 SRPK2 RBM22 NM_ Gene Name Gene Symbol Accession Synonym

251 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3457947 chr12 -3543411 chr14 55275319 55316417 +3514488 1.05 chr13 72594776 - 726585772494749 1.05 chr2 50826009 50927014 + 1.05 96843277 96864841 1.05 3877776 chr20 + 16645421 16670916 1.05 3227574 chr9 - 133123292 133147120 1.05 2844479 chr5 + 179166014 179198853 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 1 // DDX26 // DDX26 1 // DKFZp781B109 // DKFZp781B109 // FLJ13768 // FLJ13780 // FLJ45876 // // TIP5 KIAA0314 WALp3 // MGC105088 // MGC117168 // S164 RNPC7 DBI- // // DICE1 DDX26A // DKFZP434B105 // // INT6 HDB Notch12 // ACDP3 // DKFZp43411016 FLJ20018 MGC24807 // MGC24807 MGC45309 C9orf59 // // C9orf59 FLJ00024 35 // // OSIL A170 // p60 ZIP3 // PDB3 p62B // p62 // 013449 021239 012141 017623 003092 015697FLJ26072 // CL640 2775965 chr4 - 84404005 84424988 1.05 033387 003900 NM_ // 001039937 NM_ // 001039938 NM_ XM_ // 001127059 NM_ // NM_ 199078 NM_ // NM_ 198220 40 NM_

45 BAZ2A NM_ SNRPB2 COQ2 NM_ FAM78A NM_ SQSTM1 // SQSTM1 OSIL

55 RNA binding motif protein 25 RBM25 6 subunit complex integrator NM_ INTS6 cyclin M3 CNNM3 bromodomain adjacent to zinc 2A domain, finger small nuclear ribonucleoprotein ribonucleoprotein nuclear small B" polypeptide coenzyme Q2 homolog, homolog, Q2 coenzyme prenyltransferase family with sequence similarity similarity sequence with family A member 78, sequestosome 1 sequestosome Gene Name Gene Symbol Accession Synonym

252 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3729172 chr17 + 55052021 55127299 1.05 2957596 chr63012064 - chr7 53179349 + 53321902 1.05 90002707 90677837 1.05 3809324 chr18 - 52334063 52469773 1.05 2881187 chr5 - 149412410 149473128 1.05 3421300 chr12 + 67488176 67525479 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 17 // 30 1 // (continued) 2 3293840 chr10 - 73457514 73518527 1.05 FMS // CD115 // // CD115 FMS CHC17 // CLH- // CHC17 // // Hc CLTCL2 KIAA0034 HELO1 // RP3- // HELO1 483K16.1 // dJ483K16.1 // KIAA0834 PFTAIRE1 TXNL // Txl // TXNL C- // // FIM2 CSFR FMS // TXL- TRP32 35 HDMX // // hdm2 MGC71221 014767 testican- 004859 021814 012395 005211 004786 002392 006879 006882

40 NM_ // NM_ // 006878 NM_ // NM_ // 006881 NM_

45 NUMA1SPOCK2 006185 NM NUMA NM_ 3380901 chr11 - 71389909 71469367 1.05 ELOVL5 NM_ CSF1R NM_ MDM2

50 fms) fms) like 1 like TXNL1 NM_

55 osteonectin, cwcv and and cwcv osteonectin, like domains clathrin, heavy chain (Hc) chain heavy clathrin, CLTC NM_ PFTAIRE protein kinase 1 kinase protein PFTAIRE apparatus mitotic nuclear PFTK1 1 protein sparc/ kazal- 2 (testican) proteoglycan NM_ like, yeast) like, ELOVL family member 5, fatty chain of long elongation SUR4/Elo3- (FEN1/Elo2, acids thioredoxin- colony stimulating factor 1 factor stimulating colony McDonough formerly receptor, (v- viral sarcoma feline homolog oncogene Mdm2, transformed 3T3 cell cell 3T3 transformed Mdm2, binding p53 2, minute double (mouse) protein Gene Name Gene Symbol Accession Synonym

253 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2615600 chr3 + 31544326 31662283 1.05 2655113 chr3 +3427767 chr12 184836105 184882100 + 1.05 97395927 97502543 1.05 3335465 chr11 + 65162171 65174965 1.05 3336696 chr11 + 66643299 66782124 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) B ABC27 // ABC50 // ABC27 2901687 chr6 + 30647103 30667268 1.05 FLJ90106 // SIMP // // SIMP // FLJ90106 STT3- DRE1 // FLJ25796 // FLJ25796 // DRE1 // FLJ10201 // FLJ12841 // FLJ13308 KIAA1197 // // LAP2 CMD1T // MGC61508 // TP PRO0868 MGC102688 // MGC102688 SPA1 // MGC17037 35 // CXXC8 DKFZP434M1735 // // FBL7 FBL11 // // FLJ00115 // FLJ46431 // JHDM1A LILINA // KIAA1004 178862 017644 003276 006747 012308 NM_ // 001025091 001090 NM NM_ // NM_ 018023 NM_ // 001032283 NM_ // 001032284 NM_ 40 NM_ // NM_ 153253

45 ABCF1 STT3B NM_ KLHL24 // KLHL24 YEATS2 SIPA1 FBXL11 NM_

50 rich repeat repeat rich

55 induced proliferation- induced like 24 (Drosophila) // binding cassette,sub- box and leucine- and box ATP- family F (GCN20), member 1 member F (GCN20), family thymopoietin the of subunit STT3, oligosoccharyltransferase B (S. homolog complex, cerevisiae) TMPO kelch- 2 containing domain YEATS signal- 1 gene associated protein 11 protein F- Gene Name Gene Symbol Accession Synonym

254 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3228463 chr9 - 134962931 135014381 1.05 3909553 chr20 - 49436909 49603743 1.05 3965314 chr22 - 48552694 48636916 1.05 2768468 chr4 - 48194140 48272015 1.05 2499158 chr2 + 108702376 108768725 1.05 3234760 chr10 + 10544225 11418680 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) DRA1 2903189 chr6 + 32496972 32520923 1.05 FLJ20922 // RGF // // // RGF FLJ20922 RaIGEF KIAA0611 // NFAT1 // NFAT1 KIAA0611 NFATP // BRL // BRPF1 // // BRPF2 DKFZp686F0325 DKFZp686E205 // DKFZp686E205 // FLJ16177 KIAA0826 NUP358 // TRP1 // // TRP1 NUP358 TRP2 35 3 ETR- // BRUNOL3 NAPOR // 032638 // NFE1B MGC2306 2694314 chr3 - 129675850 129700720 1.05 006266 007114 ARA160 2681157 chr3 - 69151671 69184154 1.05 012340 014577 005308 GPRK5 015030 3267036 chr10 + 120957193 121256088 1.05 019111 HLA- 006267 NM_ 001042368 NM_ NM_ // NM_ 173091 XM_ // 001134434 XM_ // 001134456 NM_ NM_ 40 NM_ // 001025076 NM_ // 001025077 006561 NM

45 DRA NM_ RALGDS TMF1 NM_ NFATC2 GRK5 NM_ HLA- // RANBP2 RGPD4 CUGBP2

50 coupled receptor receptor coupled 55 like FRYL GATA binding protein 2 protein binding GATA GATA2 NM_ ral guanine nucleotide nucleotide guanine ral stimulator dissociation TATA element modulatory modulatory element TATA 1 factor nuclear factor of activated T- of activated factor nuclear calcineurin- cytoplasmic, cells, 2 dependent bromodomain containing 1 containing bromodomain BRD1 NM_ FRY- G protein- G kinase 5 major histocompatibility DR II, class complex, 2 protein binding RAN CUG triplet repeat, RNA binding binding RNA repeat, triplet CUG 2 protein Gene Name Gene Symbol Accession Synonym

255 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3610804 chr15 +2525852 97010298 chr2 97320602 + 1.05 3145020 chr8 210575559 210637315 1.05 - 95569109 95634851 1.05 2458921 chr1 - 224865889 225014518 1.05 2855501 chr5 - 43324231 43349337 1.05 2834093 chr5 + 145754916 145871713 1.05 3764103 chr17 - 53421412 53439635 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 B // B (continued) CD221 // IGFIR // // IGFIR CD221 // JTK13 // MGC142170 // MGC142172 MGC18216 // RPE2- MGC2636 // CCR9 // CCR10 1 D6 // // CMKBR9 // // MGC126678 hD6 // MGC138250 // DKFZP4341116 // DKFZp781B2117 // MGC138493 // MGC141940 MSTP054 IP3K // IP3K- // IP3K PIG37 HMGCS // HMGCS MGC90332 CA150 // CA150 // MGC133200 TAF2S ASF // MGC5228 // // MGC5228 // ASF // SF2p33 // SF2 SRp30a 35 DKFZp76181514 2659887 chr3 + 198960821 198996244 1.05 000875 006916 001296 015496 002221 002130 006706 006924 032288 NM_ // NM_ // 199229 NM_ NM_ // NM_ 183009 NM_ // 001040006 NM_ NM_ // 001078166 NM_ 40 NM_ // 001011537 NM_

45 RPE // CCBP2 RPE IGF1R NM_ ITPKB NM_ HMGCS1 NM_ TCERG1 SFRS1 FYTTD1 50 serine- 3- trisphosphate 3- trisphosphate methylglutaryl- phosphate- 3- three domain

55 5- like growth factor 1 factor growth like two- hydroxy- ribulose- KIAA1429 K1AA1429 epimerase // chemokine binding binding // chemokine epimerase 2 protein insulin- receptor inositol 1,4,5- kinase B Coenzymesynthase A 1 (soluble) 3- transcription elongation elongation transcription 1 regulator rich 1 (splicing factor 2, alternate 2, alternate factor 1 (splicing rich factor) splicing splicing factor, arginine/ factor, splicing forty- 1 containing Gene Name Gene Symbol Accession Synonym

256 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2800906 chr5 + 7922217 7954221 1.05 2421995 chr1 - 89419435 89437211 1.05 3082248 chr7 - 158205107 158355198 1.05 3177563 chr9 + 87733620 87828205 1.05 3729294 chr17 + 55325239 55429105 1.05 3678083 chr16 - 4343041 4406954 1.05 3920566 chr21 + 37661116 37857051 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 30 (continued) MGC129643 // MGC129643 MSR Mpa2 // FLJ38822 // // FLJ38822 Mpa2 GBP4L CHR2SYT // ESYT2 // ESYT2 CHR2SYT KIAA1228 // FLJ21613 // FLJ21613 // FLJ22643 bA379P1.1 PS6K // S6K // S6K1 // S6K1 // S6K PS6K p70 // STK14A // p70- // (S6K)-alpha alpha p70- // S6K 0610011B16Rik // 0610011B16Rik // FLJ22021 CRN7 // FLJ44188 35 // // DYRK1 DYRK // MNB // HP86 MNBH 003291 FLJ40359 3499453 chr13 + 101981581 102131173 1.05 002454 052941 020728 024635 003161 024535 001396 30436 // 130437 NM_ // NM_ 024010 NM_ 207398 // NM 40 NM_ // NM_ // 101395 NM_ NM_ 130438 // NM

45 MTRR GBP4 // GBP7 GBP4 FAM62B NM_ MAK10 NM_ RPS6KB1 NM_ DYRK1A 50 N- acid

55 specificity specificity methyltatrahydrofolate- tripeptidyl peptidase II peptidase tripeptidyl TPP2 NM_ 5- homocysteine homocysteine reductase methyltransferase guanylate binding protein 4 // 4 protein binding guanylate 7 protein binding guanylate family with sequence similarity similarity sequence with family containing) domain (C2 62 member B MAK10 homolog, amino- homolog, MAK10 (S. subunit, acetyltransferase cerevisiae) ribosomal protein S6 kinase, S6 kinase, protein ribosomal 1 polypeptide 70kDa, coronin 7 CORO7 NM_ dual- tyrosine-(Y)-phosphorylation 1A kinase regulated Gene Name Gene Symbol Accession Synonym

257 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3322048 chr11 +3724782 16716744 chr17 16734468 1.05 + 43082272 43117868 1.05 2972310 chr6 - 122804811 122948968 1.05 2817053 chr53844238 + chr19 77691978 + 77812317 63740597 1.05 63753931 1.05 3901696 chr202586603 - chr2 24934882 - 24987616 1.05 171538552 171796060 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 2 30 (continued) IMAGE145052 // // IMAGE145052 // MGC117265 SMAP // TDE1L KIAA1253 // TMS- TDE2 // // // IPOB IMB1 // MGC2155 Impnb // MGC2156 // NTF97 // MGC2157 SCAMP // // SCAMP SCAMP37 // KAP1 FLJ29029 B // TF1 // RNF96 TIF1B 35 // ACAS2L // AceCS2L // FLJ45659 MGC33843 PKU- // KIAA0137 BETA 014267 020755 002265 052822 005762 032501 012290

40 NM_ // NM_ 004866

45 C11orf58 NM_ SCAMP1 ACSS1 NM_

50 containing 28 TRIM28 NM_

55 like kinase 1kinase like TLK1 NM_ CoA synthetase short- serine incorporator 1 SERINC1 NM_ karyopherin (importin) beta 1 beta (importin) karyopherin KPNB1 NM_ tripartite motif- tripartite chromosome 11 open reading frame 58 tousled- membrane carrier secretory 1 protein acyl- chain family member 1 member family chain Gene Name Gene Symbol Accession Synonym

258 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3626704 chr15 - 56949072 57013564 1.05 3886050 chr20 +2544238 chr2 41519932 41526301 - 1.05 24279241 24436906 1.05 3654859 chr16 + 28817718 28756043 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) DKFZp762G052 // // DKFZp762G052 // FLJ10005 // Met FLJ13213 B52 // MGC5045 // MGC5045 // B52 SRP55 // KIAA1256 SH3D1B // SH3P18 // SWAP SWA // Q6 // QSOX1Q6 2369950 chr1 + 178353067 178436483 1.05 35 // // A2LG // A2D - A2RP // A2LP 017968 002444 - 3979659 chrX + 64804248 64878488 1.05 006275 006277 147152 002826 207434 007245 145714 48415 // 148416 NM_ // 001013843 NM_ // NM_ 024755 NM_ // NM_ // 019595 NM_ NM_ // 001004128 NM_ 40 NM_ // XM_ // 001127543 NM_ // NM_ // 017492 NM_ // NM_ // 148414 NM_ NM_

45 SLTM SFRS6 NM_ QSCN6 // FLJ23867 FLJ46363 // FLJ46363 ATXN2L

50 serine-

55 like, transcription transcription like, like intersectin 2intersectin ITSN2 moesinSAFB- modulator MSN NM_ rich 6 splicing factor, arginine/ factor, splicing quiescin Q6 quiescin hypothetical FLJ46363 // ataxin ataxin // FLJ46363 hypothetical 2- Gene Name Gene Symbol Accession Synonym

259 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3110171 chr8 + 104102441 104171800 1.05 2672532 chr3 -2515050 47032936 chr2 47180418 1.05 + 171457150 171551619 1.05 3309755 chr10 - 121568302 121642742 1.05 2370991 chr1 + 181075106 181123738 1.05 Transcript Transcript ID Cluster 3808854 chr18 - 51010981 51506795 1.05 Human ST Exon 1.0 1 // 30 (continued) ATP6C // ATP6D // ATP6D // ATP6C // // VATC FLJ20057 Vma5 FLJ16420 // FLJ16420 // FLJ22472 // FLJ23184 // HIF- FLJ45883 // HSPC069 HYPB KIAA1732 // // DKFZP434D156 // FLJ13139 GOLPH6 // // GRASP55 GRS2 3alpha- // p59 // // // RDH15 HSD // RETSDR8 RDHL FLJ13081 // FLJ13081 FLJ36756 DDX9 // LKP // NDH // LKP // DDX9 NDHII // RHA // II 35 // ITF2 // E2-2 // MGC149723 // MGC149724 // SEF2-1 // SEF2 // SEF2- SEF2-1A 1B 015530 001695 014159 024834 001357 003199 199204

40 NM_ // NM_ // 005771 NO_ NM_ // 001007254 NM_

45 GORASP2 // DHRS9 ATP6V1C1 C10orf119 NM_ DHX9 NM_

50 His) box box His) Ala- reductase reductase Glu-

55 golgi reassembly stacking // 55kDa 2, protein dehydrogenase/ 9 member (SDR family) (chicken) of myb1 target transporting, H+ ATPase, subunit V1 42kDa, lysosomal TOM1C1 005488 NM FLJ33404 3944084 chr22 + 34025845 34073962 1.05 SET domain containing 2 containing domain SET SETD2 NM_ chromosome 10 open reading frame 119 DEAH (Asp- polypeptide 9 polypeptide transcription factor 4 factor transcription TCF4 NM_ Gene Name Gene Symbol Accession Synonym

260 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3589458 chr15 + 37614946 37678406 1.05 3139722 chr8 - 71184397 71478626 1.05 3471005 chr12 - 108852000 108918536 1.05 3916576 chr21 +2712040 chr3 26028762 26066641 - 1.05 196476779 196645492 1.05 2905069 chr6 + 36518349 36566874 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 // B2 (continued) 2 // T1F2 2 // 2 // 2 // KIAA1093 3946192 chr22 + 38770332 39061757 1.05 THBS // TSP // // TSP THBS TSP1 GRIP1 // GRIP1 // MGC138808 NCoA- CAT- DKFZp686G01261 // KIAA0148 // MGC760 E4TF1-60 // E4TF1-60 // // NFT2 E4TF1A NRF2A // // NRF2 // E4TF1B // E4TF1 GABPB1 CNT- // ACAP2 KIAA0041 35 // C6orf69 // MGC14254 dJ108K11.3 015088 003246 006540 014776 057170 002040 012287 022452 // FLJ11618 FBS 3656362 chr16 + 30577810 30590035 1.05 173562 005990 // PRO2729 LOK 2887048 chr5 - 171401689 171547855 1.05 NM_ // 001024843 NM_ NM_ // NM_ // 057169 NM_ // NM_ 139201 40 NM_ NR_ // - 002723

45 TNRC6B GIT2 GABPA // GABPAP KCTD20STK10 NM_ NM_

50 coupled receptor receptor coupled 55 threonine kinase 10 GA trinucleotide repeat containing containing repeat trinucleotide 6B thrombaspondin 1thrombaspondin THBS1 NM_ vimentin 2 coactivator receptor nuclear NCOA2 NM_ VIM 003380 NM FLJ36605 3236958 chr10 + 17296705 17357733 1.05 centaurin, beta 2 beta centaurin, 1fibrosin CENTB2 NM_ FBS1 NM_ G protein- G kinase interactor 2 serine/ transcription protein binding // 60kDa subunit alpha factor, transcription protein binding GA subunit alpha factor, pseudogene potassium channel channel potassium tetramerisation domain 20 containing Gene Name Gene Symbol Accession Synonym

261 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3770345 chr17 - 70117621 70131474 1.05 2353477 chr12815043 + chr53834089 + 116706775 chr19 116754386 1.05 72148176 + 72245960 1.05 46460006 46505508 1.05 2773756 chr4 - 767868072823880 76869171 chr5 1.05 + 110587242 110854177 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) GR // // GR AP5 // CD300LE // CLM2 // CLM2 // CD300LE // CCA IREM2 MGC3285 // // MGC3285 MGC51750 // // KPNB2 IPO2 MIP // MIP1 // E1B- // E1BAP5 FLJ12944 35 // // MGC119326 - // MGC119329 // ROR1 // NR1F1 // ROR3 // ROR2 RZRA CaMK- MGC36771 1 181449 000701 002270 144733 144732 012297 203505 024611 134260 134262 001744 005109 OSR1 // KIAA1101 2617579 chr3 + 38182030 38271979 1.05 NM_ // NM_ 001999 NM_ // NM_ 001001586 NM_ 153188 // NM NM_ // NM_ // NM_ 44734 // 007040 NM_ 40 NM_ // NM_ // 203504 NM_ // NM_ // 001018089 NM_ // NM_ // 002943 NM_ // NM_ // 134261 NM_

45 CD300E // CD300E FBN2 ATP1A1 HNRPUL1 CAMK4 NM_ G3BP2 // // G3BP2 NARG2 // RORA

50 like 1 like dependent dependent stress responsive 1 responsive stress OXSR1 NM_

55 calmodulin- related orphan receptor A receptor orphan related transportin 1transportin nuclear heterogeneous U- ribonucleoprotein 2 fibrillin // TNPO1 molecule CD300e contractural (congenital arachnodactyly) calcium/ oxidative- ATPase, Na+/K+ transporting, transporting, Na+/K+ ATPase, polypeptide 1 alpha protein kinase IV kinase protein GTPase activating protein (SH3 (SH3 protein activating GTPase 2 // protein binding domain) // 2 regulated receptor NMDA RAR- Gene Name Gene Symbol Accession Synonym

262 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2831124 chr5 + 138505686 138695245 1.05 2720181 chr4 + 17225344 17244808 1.05 3830002 chr19 + 40161899 40210121 1.05 3076340 chr7 - 139994192 140274640 1.05 3422326 chr12 + 70519754 70604360 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) raf 1 // BRAF1 // // // BRAF1 raf 1 RBBP2 // RBP2 // RBBP2 3439603 // chr12DKFZp686K0542 DKFZp688K23100 // KIAA0723 // -MGC9105 259504 368944 1.05 1500003D12Rik // 1500003D12Rik // DKFZP434N185 EG1 // magicin HRS // SRP40 HRS // FLJ22411 3542207 // FLJ90346 chr14KIAA1533 + 69263363 69308465 1.05 B- // MGC126806 // MGC138284 RAFB1 35 // DKFZp686M1379 // DKFZp761D0223 FLJ12085 018834 025205 006925 020895 004333 022771 000574 TO // DAF // CR 2377229 chr1 + 205561488 205607671 1.05 NM_ // 001042603 005056 NM NM_ // NM_ 199189 40 NM_ // 001039465 NM_

45 JARJD1A MED28 NM_ SFRS5 BRAF NM_ TBC1D15 NM_ CD55 NM_

50 serine-

55 raf murine sarcoma viral viral sarcoma raf murine activating transcription factor 6 factor transcription activating ATF6 3matrin 007348 NM - MATR3 2363919 chr1 + 160002678 160208836 1.05 jumonji, AT rich interactive interactive rich AT jumonji, 1A domain GRAM domain containing 1A containing domain GRAM GRAMD1A II polymerase of RNA mediator transcription,subunit 28 NM_ (S. cerevisiae) homolog rich 5 splicing factor, arginine/ factor, splicing v- B1 homolog oncogene TBC1 domain family, member member family, domain TBC1 15 CD55 molecule, decay decay molecule, CD55 for factor accelerating blood (Cromer complement group) Gene Name Gene Symbol Accession Synonym

263 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3427820 chr12 + 97511471 97519906 1.05 2702307 chr3 -3722417 158305077 chr17 158361233 1.05 +2405192 38563761 chr1 38719231 1.05 - 33012453 33056331 1.05 3558375 chr14 - 24169951 24173308 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 1 // 1 30 B // 48 // 48 (continued) cl. 001 // // 001 OK/SW- PHC BM- // ania- PRO1073 1A1-3B // // M17S2 KIAA0049 // MIG19 TYRRS // CMTDIC YTS YRS // // 35 // CGL- CCP1 CSP- // CGL1 // // CTLA1 CSPB HLP // // CTSGL1 SECT 213612 005888 020307 005899 003680 004131 NM_ // NM_ // 002635 NM_ // NM_ 213611 40 XM_ // 001124650 XM_ // 001124827 XM_ // 001127781 NM_ // NM_ NM // 031858 031862

45 SLC25A3 GZMB NM_

50 lymphocyte- 55 rtRNA synthetase rtRNA YARS NM_ neighbor 1of BRCA1 gene neighbor NBR1 tyrosyl- 25 family carrier solute carrier, (mitochondrial 3 member carrier), phosphate cyclin L1 CCNL1 NM_ associated serine esterase 1) granzyme B (granzyme 2, 2, (granzyme B granzyme cytotoxic T- Gene Name Gene Symbol Accession Synonym

264 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2356115 chr1 + 144149846 144164251 1.05 3277662 chr10 - 11984615 12125155 1.05 4002173 chrX - 20077954 20254253 1.05 3896370 chr20 - 5473033 5546357 1.05 2986084 chr6 - 169845929 169866056 1.05 3693673 chr16 - 57111094 57236550 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 3 // ISPK- (continued) 005 //CDC39 // EST01027 // EST01027 HHCPA78 // THIF // VDUP1 DKFZP434D222 // // DKFZP434D222 // KIAA1408 HUPF2 // MGC138834 // // MGC138835 CLS // HU- // CLS 1 // MAPKAPK1B // // MAPKAPK1B // 1 // // RSK MRX19 S6K- // RSK2 RSK2 p90- // alpha3 pp90RSK2 // FLJ11085 // FLJ11085 // KIAA1434 MGC26147 MGC50828 // FLJ10975 // MGC111009 3336857XAP135 chr11 + 66812660 66826524 1.05 35 AD- // DKFZp686E0722 // FLJ90644 NOT1 // KIAA1007 NOT1H // 006472 015542 004586 019593 207354 018288 016284 NM_ // NM_ 080599 XM_ // 001129739 NM_ NM_ // NM_ 133325 40 NM_ // NM_ 206999

45 UPF2 RPS6KA3 NM_ ANKRD13D CNOT1

55 NOT transcription transcription NOT thioredoxin interacting protein interacting thioredoxin TXNIP NM_ UPF2 regulator of nonsense nonsense of regulator UPF2 transcripts homolog (yeast) ribosomal protein 56 kinase, kinase, 56 protein ribosomal 3 polypeptide 90kDa, PHD finger protein 10 protein finger PHD KIAA1434protein hypothetical PHF10 RP5-1022P6.2 NM_ ankyrin repeat domain 13 13 domain repeat ankyrin D member family, CCR4- 1 subunit complex, Gene Name Gene Symbol Accession Synonym

265 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3501661 chr13 + 110565635 110756075 1.05 2975287 chr6 - 135314409 135417715 1.05 3253880 chr10 + 80777230 80785093 1.05 3884830 chr20 + 36866338 36985066 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 D // (continued) PIX // PIX // 1 a ERFS // 1 a // BETA- COOL1 // // DKFZp761K1021 // KIAA0142 // KIAA0412 // // P50 Nbla10314 // P85 // P50BP // P85COOL1 // PAK3 // P85SPR PIXB DKFZp686L13262 DKFZp686L13262 // EF- // HSPC276 // HBS1 // ALDH12 // DJ352A20.2 // DKFZp779D2315 FLJ40431 2426385 chr1 - 107914594 108309371 1.05 FLJ90798 // FLJ90798 MGC117207 CYP3 // Cyp- // CYP3 35 // ANKRD4 TIMAP // KIAA0823 003899 006620 170771 006113 000859 - 2815965 chr5 + 74668800 74700136 1.05 005729 015568 NM_ // NM_ 145735 40 NM_ // NM_ // 022568 NM_ NM. // 001079874 NM_

45 ARHGEF7 HBS1L // // HBS1L ALDH8A1 HMGCR NM_ PPIF NM_ PPP1R16B NM_

50 methylglutaryl- 3- 55 like (S. cerevisiae) // cerevisiae) (S. like hydroxy- vav 3 oncogenevav VAV3 nucleotide guanine Rho 7 (GEF) factor exchange chloride intracellular channel 1 CUC1HBS1- 8 dehydrogenase aldehyde A1 member family, NM 001288 // NCC27 G6 2949330 chr6 - 31806365 31815144 1.05 Coenzymereductase A 3- peptidylprolyl isomerase F isomerase peptidylprolyl F) (cyclophilin protein phosphatase 1, phosphatase protein subunit (inhibitor) regulatory 16B Gene Name Gene Symbol Accession Synonym

266 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3034027 chr7 +3254521 156799667 chr10 156902887 1.05 + 82203922 82272901 1.05 3483348 chr13 + 28125188 28151050 1.05 2745646 chr4 + 144616165 144697227 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 2 // HSJ2 // HSJ2 2 // TM4F2 // DKFZp566D0824 // // DKFZp566D0824 FLJ42837 // HHDJ1 // HSJ- // MGC1152 II MGC117297 DC- // MGC11352 TM4SF14 C13orf12 // C13orf12 // PNAS- HSPC014 110 // UMP1 35 // SNF2H // ISWI // hISWI WCRF135 hSNF2H // 005494 016107 FLJ41312 030927 2852333 chr5 - 32390101 32537319 1.05 015932 003601

40 NM_ // NM_ 058246

45 DNAJB6 SMARCA5 NM_

55 zinc finger RNA binding protein binding RNA finger zinc ZFR NM_ tetraspanin 14tetraspanin TSPAN14 NM_ DnaJ (Hsp40) homolog, 6 B, member subfamily proteasome maturation protein maturation proteasome POMP NM_ SWI/SNF related, matrix matrix related, SWI/SNF dependent actin associated, of chromatin, regulator 5 member a, subfamily Gene Name Gene Symbol Accession Synonym

267 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3470793 chr12 - 108370845 108399528 1.05 3020192 chr7 + 115637811 115743800 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 1BLC3 3672830 chr16 + 85982917 85996864 1.05 2 // TESTIN FLJ41739 // FLJ41739 // MSTP028 ULRO61 DKFZP58682022 // // DKFZP58682022 TESS // MGC1146 TESS- // 35 MGC99675 3814063 chr18 - 72853742 73023063 1.05 001987 TEL/ABL // TEL 3405032 chr12 + 11645490 11939588 1.05 031954 006521 // TFEA RCCP2 152272 Mac2981 4007734 chrX 3089853 - chr8 48771186 + 48787973 1.05 23157105 23176288 1.05 022818 MAP1A/ 015641 NM_ // NM_ 152829 40 NM_ // 001025081 NM_ // 001025090 NM_ // 001025092 NM_ // 001025094 NM_ // 001025098 NM_ // 001025100 NM_ // 001025101 002385 NM

45 ETV6 NM_ KCTD10 NM_ TFE3 NM_ MAP1LC3B NM_ TES

50 associated protein protein associated

55 ets variant gene 6 (TEL (TEL 6 gene variant ets oncogene) CHMP family, memberCHMP family, 7 channel potassium tetramerisation domain CHMP7 10 containing NM_ transcription factor binding to binding factor transcription 3 enhancer IGHM microtubule- 3 beta chain light 1 myelin basic protein MBP LIM (3 transcript derived testis domains) Gene Name Gene Symbol Accession Synonym

268 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3375245 chr11 -2621827 chr3 60823513 60857553 + 1.05 48930742 48997971 1.05 3475511 chr12 - 121267461 121277963 1.05 3475324 chr12 - 120698553 120716624 1.05 2616317 chr3 + 33743952 33886195 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 DDB1 BF (continued) S // 76 // SLP76 76 2886595 chr5 - 169607157 169657789 1.05 DDBA // UV- DDBA // XPCE XAP1 // // XPE- XPE AR12 // FLJ10938 // // FLJ10938 AR12 // FLJ33921 TRIAD1 MOX44 // TSPAN25 // MOX44 2351572 chr1 + 111215352 111296983 1.05 NR111DIABLO- // FLJ10537 // SMAC FLJ25049 3452818 SMAC3 // chr12 - 46521596 46606823 1.05 ARHF // FLJ20247 // FLJ20247 ARHF // RIF 35 DRIP4 // // Alix AIP1 // HP95 // MGC17003 001923 006321 001731 - 000560 3465409 chr12 - 90902887 91063960 1.05 000376 019887 138930 005565 SLP- 019034 013374 XM_ // 001128974 XM_ // 001128983 NM_ NM_ // NM_ 001040033 40 NM_ II NM_ 001017535 NM_ // NM_ // 138929 NM_

45 DDB1 BTG1 NM_ VDR LCP2 NM_ RHOF NM_ PDCD61P NM_

55 specific DNA binding cell translocation gene 1, anti- 1, gene translocation cell ariadne homolog 2 (Drosophila) homolog ariadne ARIH2 NM_ damage- 127kDa 1, protein CD53 moleculeCD53 CD53 diablo homolog (Drosophila) homolog diablo DIABLO B- proliferative vitamin D (1,25- (1,25- D vitamin D3) receptor dihydroxyvitamin lymphocyte cytosolic protein 2 protein cytosolic lymphocyte containing domain (SH2 76kDa) of protein leukocyte ras homolog gene family, family, gene homolog ras filopodia) F (in member programmed cell death 6 6 death cell programmed protein interacting Gene Name Gene Symbol Accession Synonym

269 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3690084 chr16 -3518496 chr13 45546783 45565155 - 1.05 76500672 76799212 1.05 3653398 chr16 +3671873 chr16 24583665 24748478 + 1.05 83291080 83371023 1.05 3739431 chr17 + 78630769 78653225 1.05 3009959 chr7 + 77004361 77123074 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) PEST // PEST // CPR3 // DJA2 // // DJA2 // CPR3 // DNJ3 // DNAJ PRO3015 // HIRIP4 RDJ2 DKFZp686M08244 // FLJ10106 // // FLJ13826 // FLJ21597 // FLJ21646 PAM // KIAA0916 CAGH26 // CAGH26 // OKFZp666E117 // // GW1 FLJ22043 GW182 // // KIAA1460 // MGC75384 TNRC6 // K1AA0190 UBPO // MGC2621 MGC99788 // MGC99788 // ARC92 // ACID1 // DKFZp434K0512 // P78 // MGC70671 TCBAP0758 35 PTP- PTPG1 005880 015057 020847 005153 030973 002835 941466 941466 NM_ // NM_ 014494 40 XM_ 11 NM_ // 001004431 NM_

45 DNAJA2 NM_ TNRC6A METRNL // METRNL MED25 PTPN12 NM_

55 of RNA mediator // like receptor type 12 type receptor MYC binding protein 2protein binding MYC MYCBP2 NM_ ubiquitin specific peptidase 10 peptidase specific ubiquitin USP10DnaJ (Hsp40) homolog, 2 A, member subfamily NM_ trinucleotide repeat containing containing repeat trinucleotide 6A meteorin, glial cell differentiation differentiation cell glial meteorin, regulator- transcription, Il polymerase (S. homolog 25 subunit cerevisiae) protein tyrosine phosphatase, phosphatase, tyrosine protein non- Gene Name Gene Symbol Accession Synonym

270 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3638607 chr15 - 88129142 88159617 1.05 3354174 chr11 +3816509 chr19 123997906 124011654 + 1.05 2425718 2469133 1.05 3778601 chr182531377 + chr2 9903984 + 9950012 230985008 1.05 231142598 1.05 3918635 chr21 + 33696906 33774607 1.05 2739079 chr4 + 110510304 110681811 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 33 30 5 A // A // (continued) 1 // IFGR2 // // IFGR2 1 // APN // CD13 // // CD13 APN PEPN // // LAP1 gp150 FLJ14621 // FLJ14621 // FLJ25020 // FLJ90113 // MGC129890 TB- // NIAM // DKFZP566B133 // GADD45BETA MYD118 MGC3745 // VAP- // MGC3745 VAP- // 33 hVAP- // VAP33 DKFZp686E07254 DKFZp686E07254 // FLJ00340 // FLJ34579 AF- IFNGT1 35 // MGC48822 SEC24 001150 015675 003574 003113 005534 006323 NM_ // NM_ 194434 NM_ // 001080391 NM_ 40 XM // 001130118 NM_ II 001042734 NM_

45 ANPEP NM_ GADD45B NM_ TBRG1 032811 No VAPA IFNGR2 NM_ SEC24B

50 associated associated

55 beta inducible, damage- growth arrest and DNA- and arrest growth (membrane) alanyl aminopeptidase (aminopeptidase N, microsomal M, aminopeptidase p150) CD13, aminopeptidase, SP100 nuclear antigen nuclear SP100 SP100 beta factor growth transforming 1 regulator VAMP (vesicle- VAMP protein)-associated membrane 33kDa A, protein interferon gamma receptor 2 receptor gamma interferon transducer gamma (interferon 1) SEC24 related gene family, family, gene related SEC24 B (S. cerevisiae) member Gene Name Gene Symbol Accession Synonym

271 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2714955 chr4 + 1692616 1716693 1.05 3372253 chur11 - 47444068 47543613 1.05 3238491 chr10 + 22650103 22660820 1.05 3882069 chr20 + 30871304 30901864 1.05 2553282 chr2 - 53944710 54160919 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) ERIC1 // ERIC1 // MGC117382 MGC133242 BRUNOL2 // CUG- BRUNOL2 // // CUGBP BP hNab50 // NAB50 MGC12685 // MGC12685 // RNF51 PCGF4 EB1 // MGC117374 MGC117374 // EB1 MGC129946 // 35 // FLJ21864 // KIAA0077 // MGC138374 // MGC142228 PA200 006342 006560 005180 012325 014614

40 NM_ // 001025596 NM_ // NM_ 198700

45 TACC3 NM_ CUGBP1 BMI1 NM_ MAPRE1 NM_ PSME4 NM_ coil

50 associated protein, protein, associated

55 transforming, acidic coiled- 3 protein containing CUG triplet repeat, RNA binding binding RNA repeat, triplet CUG 1 protein BM11 polycomb ring finger finger ring polycomb BM11 oncogene microtubule- 1 member family, RP/EB proteasome (prosome, (prosome, proteasome 4 subunit activator macropain) Gene Name Gene Symbol Accession Synonym

272 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2362394 chr12960010 + chr6 157215279 - 157291561 1.05 70361077 70634121 1.05 2548500 chr2 - 37331165 37405413 1.05 3443183 chr12 - 8577026 8584811 1.05 3212976 chr9 - 88092469 88159805 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 NU // (continued) NU 1FNGIP1 // // MGC9466 PYHIN2 // C6orf209 // RP11- FLJ11240 // 810122.1 bA810122.1 PKC- // EPK2 // PRKCN // PKD3 nPKC- CLECSF9 // CLECSF9 MINCLE 35 // DKFZp666B142 DKFZp686C11112 // DKFZp686F119 // // OKFZp68611269 JFP2 // PAPD6 005531 018368 005813 014358 024617 032366

40 NM_ // NM_ // 001040160 NM_ // 001040161 NM_ // 001040162 NM_ // 001040163 NM_ // 001040164 NM_ // 001040165 NM_ // 001040166 NM_

45 IF116 NM_ CLEC4E NM_ ZCCHC6 // ZCCHC6 MGC13114

50 inducible

55 type lectin domain family 4, 4, family domain lectin type LMBR1 domain containing 1 containing domain LMBR1 LMBRD1 D3 kinase protein NM_ PRKD3 NM_ interferon, gamma- interferon, protein 16 protein C- member E zinc finger, CCHC domainzinc finger, hypothetical 6 II containing MGC13114 protein Gene Name Gene Symbol Accession Synonym

273 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3940099 chr22 +3755714 chr17 23143709 - 23200243 1.05 34801544 34861069 1.05 2890148 chr5 - 178970155 178993890 1.05 3892607 chr20 + 60305485 60317305 1.05 3819543 chr19 + 8415651 8459993 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 1 3125775 chr8 - 17128912 17148758 1.05 (continued) 4 3665288 chr16 + 65783266 65790299 1.05 DKFZp781D1727 3609138 chr15 + 91227096 91387351 1.05 ADORA2 // RDC8 ADORA2 // hA2aR CRSP200 // CRSP1 // DR1P205 // // MED1 // DRIP230 // PBP // MGC71488 // PPARGBP // RB18A DKFZp686A15170 DKFZp686A15170 HNRPH // // // GP110 // MGC29536 DKFZp547H118 // // DKFZp547H118 HNRNPM // HNRNPM4 // HNRPM4 // HTGR1 // NAGR1 35 hCAF- // CAF1 001271 001950 E2F- 003769 SRp30c 3474502 chr12 - 119372834 119407274 1.05 000675 004774 004226 DRAK2 2593159 chr2 - 196706552 196744596 1.05 005520 007002 005968 013354 NM_ // 001042572 NM_ NM_ // NM_ 175573 NM_ // NM_ 031203 40 NM_ // NM_ 054026

45 CHD2 E2F4 NM_ HNRPH1 NM_ HNRPM CNOT7

50 9 rich SFRS9 NM_ serine- binding

55 NOT transcription transcription NOT threonine kinase 17b kinase threonine STK17B NM_ chromodomain helicase DNA DNA helicase chromodomain 2 protein binding factor, E2F transcription factor factor transcription E2F factor, p107/p130- 4, PPAR binding proteinPPAR binding serine/ PPARBP NM_ adhesion regulating molecule 1molecule regulating adhesion ADRM1 adenosine A2a receptor A2a adenosine ADORA2A NM_ arginine/ splicing heterogeneous nuclear nuclear heterogeneous H1 (H) ribonucleoprotein heterogeneous nuclear nuclear heterogeneous M ribonucleoprotein CCR4- 7 subunit complex, Gene Name Gene Symbol Accession Synonym

274 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2674242 chr3 - 49371587 49424514 1.05 2617041 chr3 + 37259518 37452233 1.05 3066818 chr7 -3246372 105625846 chr10 1057132663336801 1.05 + chr11 51202191 + 51260947 1.05 66790523 36810933 1.05 3257938 chr10 + 93673509 93821994 1.05 3791935 chr18 + 59704265 59722138 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 170 170 30 (II) 40.18 // // 40.18 (continued) 1 // MAR 1 // 2875348 chr5 - 131846280 131893043 1.05 2 // PAI2 // PAI2 2 // RMS- ARH12 // ARHA // // ARH12 // RHOH12RHO12 p230 KIAA0940 // // KIAA0940 // MGC138406 TAF // MOT1 GCP2 // GOLG // MU- 1110035014Rik // 1110035014Rik // DKFZP666B131 // MGC117256 // PBEF // NAMPT LOC646309 // ARA70 // DKFZp762E1112 // PTC3 // ELE1 RFG BETA- // BARK1 GRK2 // ARK1 // TAF172 // TAF172 // TABII170 35 // // PAI HsT1201 PAI- PLANH2 001664 003972 002078 005746 00219B IRF- 005437 020820 KIAA1415 3908631 chr20 - 46674205 46938090 1.05 002575 001619

40 NM_ // -

45 RHOA NM_ ADRBK1 M_ BTAF1 NM_ GOLGA4 NM_ PBEF1 // // PBEF1 RP11-92J19.4 PREX1 NM_ SERPINB2 NM_ 50 dependent RAC RAC dependent B cell enhancing enhancing B cell

55 cell colony enhancing enhancing colony cell B- ras homolog gene family, family, gene homolog ras member A interferon regulatory factor 1 factor regulatory interferon IRF1 4 coactivator receptor nuclear NCOA4 receptor beta, adrenergic, NM_ kinase 1 NM_ B- II, RNA polymerase BTAF1 factor- transcription TFUD associated, 170kDa(Mot1 cerevisiae) S. homolog, golgi autoantigen, golgin golgin autoantigen, golgi 4 a, subfamily pre- pre- 1 // factor 1 pseudogene factor phosphatidylinositol 3,4,5- phosphatidylinositol trisphosphate- 1 exchanger serpin peptidase inhibitor, clade clade inhibitor, peptidase serpin 2 member B (ovalbumin), Gene Name Gene Symbol Accession Synonym

275 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2982381 chr62651782 - chr3 + 160119521 160130731 1.05 171166446 171194653 1.05 2363248 chr1 + 159032527 159064855 1.05 3526378 chr13 - 112877970 112912799 1.05 3090922 chr8 + 26156860 26286261 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 alpha (continued) alpha // CCT1 // alpha CCT1 CCT- D6S230E // CCTa // TCP- 1- // Dtrp1 // FLJ32803 // // FLJ32803 Dtrp1 SEC62 // HTP1 // FUBPFBP 2419235 chr1 - 78182330 78217881 1.05 CD229 // SLAMF3 // // SLAMF3 CD229 // 19A mLY9 // hly9 CD319CRACC // // GS1 F10 // FLJ11305 // // // FLJ11305 F10 16774 MGC B55A // FLJ26613 // // // FLJ26613 B55A // MGC52248 PR55A // PR52A 35 - 2434971 chr1 - 149578882 149586373 1.05 018036 FLJ10242 004145 MYR5 // CELIAC4 3823982 030752 3578278 chr19 chr14 + - 17047591 95817349 17185088 95900740 1.05 1.05 003262 020801 TLIMP // KIAA1376 2866704 chr5 - 90700311 90782084 1.05 021181 017896 TWA1 018386 3893072 chr20 + 61039681 61050570 1.05 002717 000449 NM_ // 001008897 NM_ NM_ 001033667 NM_ 11 // // 002348 NM_ 40 NM_ // NM_ 001025603

45 C14orf103 NM_ LY9 // SLAMF7 // LY9 C20orf11 NM_ PPP2R2A NM_ RFX5

55 complex 1 TCP1 myosin IXBt- MYO9B NM_ translocation protein 1protein translocation (FUSE) element upstream far 1 protein binding TLOC1 NM_ chromosome 14 open reading frame 103 arrestindomain containing 3 ARRDC3 NM_ lymphocyte antigen 9 // SLAM // SLAM 9 antigen lymphocyte 7 member family PCI domain containing 2 PCID2 NM_ chromosome 20 open reading frame 11 expression) protein 2A), (formerly 2 phosphatase B, alpha subunit regulatory isoform regulatory factor X, 5 (influences 5 (influences X, factor regulatory classHLA II Gene Name Gene Symbol Accession Synonym

276 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3086206 chr8 + 11690497 11740987 1.05 3474228 chr12 - 119017289 119039689 1.05 3702293 chr16 - 82644885 82708018 1.05 2401275 chr1 - 23486545 23543926 1.05 2812435 chr5 + 65258079 65451372 1.05 3907830 chr20 - 44426906 44495031 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 2 // 2 12 // 12 CED12 // 1 ray // RAB1C // // RAB1C ray DGPT // ERG9 // // ERG9 DGPT SS // SQS H- RAY KIAA0091 // // KIAA0091 // MGC138711 // 138712 MGC S1P // // PCSK8 SKI- FLJ25714 // FLJ25714 HNRNPR // hnRNP- R ERBIN // LAP2 // // // LAP2 ERBIN MCH2 35 //-MAN1B CED- ELMO- 2353881 // FLJ11656 KIAA1834 chr1 + 117689854 117931990 1.05 004462 002971 2665199 chr3 - 18364435 18462086 1.05 006861 003791 005826 018695 032992 003902 006699 133171 NM_ // NM_ 201268 NM_ // 001006600 NM_ // NM_ // 001226 NM_ 40 NM_ NM_ // - NM_ // NM_ 182764

45 FDFT1 NM_ RAB35 NM_ MBTPS1 HNRPR NM_ ERBS21P // CASP6 FUBP1 FUBP1 // MAN1A2 UCA1

50 related related bound transcription transcription bound

55 diphosphate SATB homeobox 1homeobox SATB SATB1 NM_ famesyl- 1 farnesyltransferase RAB35, member RAS member RAB35, family oncogene membrane- 1 site peptidase, factor heterogeneous nuclear nuclear heterogeneous R ribonucleoprotein engulfment and cell motility 2 motility cell and engulfment ELMO2 // protein interacting erbb2 apoptosis- 6, caspase cysteine peptidase cysteine mannosidase, alpha, class 1A, class alpha, mannosidase, cancer urothelial 2 // member associated 1 Gene Name Gene Symbol Accession Synonym

277 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2406677 chr1 - 36577822 36626062 1.05 3320301 chr11 + 10684027 10774985 1.05 2440143 chr1 -3428131 chr12 158525015 + 158580073 1.05 99185070 99260564 1.05 Transcript Transcript ID Cluster 3618736 chr15 - 36567598 36809973 1.05 Human ST Exon 1.0

30 GEFI// GEFI// // GEFII (continued) MGC4796 // RP11- // RP11- MGC4796 // SHIK 268J15.4 // 4.1R // SgK495 HE // EL1 KIAA0155 // // KIAA0155 // TSBP // SH2BP1 p15D // p150TSP // // MGC99627 MTO2// MTU1 // // // TRMT1 TRMT FLJ26320 // HEP- FLJ26320 // // D1S2223E COP // PMP1 // HK33 // // PXF PMPI PXMP1 // CVAK104 // FLJ10074 KIAA1360 PC4 // TIS7PC4 3019519 chr7 + 111835465 111903788 1.05 35 CALDAG- CALDAG- // MGC129998 // MGC129999 V // RASGRP // hRasGRP1 032017 014633 004371 017988 001550 005739 NM_ // NM_ // 004437 203342 NM_ // NM_ 203343 NM_ // NM_ 018006 NM_ // NM_ 002857 40 NM_ // 001007245 NM_

45 STK40 // STK40 EPB41 CTR9 // TRMU // CTR9 COPA // PEX19 IFRD 1 IFRD RASGRP1 NM_ 50 2- regulated) related 55 threonine kinase 40 // 40 kinase threonine like 2 (S. cerevisiae) 2 like SCYL2 NM_ serine/ protein membrane erythrocyte RH- 1, (elliptocytosis 4.1 band linked) SCY1- II polymerase Paf1/RNA Ctr9, complex component, homolog 5- // tRNA cerevisiae) (S. methylaminomethyl- thiouridylate methyltransferase coatomer protein complex, complex, protein coatomer // peroxisomal alpha subunit 19 factor biogenesis RAS guanyl releasing protein 1 protein releasing guanyl RAS and DAG- (calcium interferon- developmental regulator 1 regulator developmental Gene Name Gene Symbol Accession Synonym

278 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2911944 chr6 + 64403666 64547188 1.05 3698919 chr16 - 73015604 73209803 1.05 3553228 chr14 + 102053947 102266629 1.05 2464499 chr1 - 243078713 243094575 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 A

30 // 1 Sema Sema (continued) Sema Y2 Sema 3 // WIPI3 3 3775157 chr17 - 78165748 78199803 1.05 1 // ESL- 1 // CFR- // FLJ23319 // MG- FLJ23967 // // MG160 160 SPEC1 // // SCIP1 m- // SEMAY // m- Y // KIAA0244 // MGC142210 MGC142212 COREST // RCOR // KIAA0071 // RSTS // RTSCBP 3677795 chr16 - 3715075 3870713 1.05 35 SAF- HNRNPU // // U21.1 012257 FLJ16340 3018420 chr7 + 106596679 106630194 1.05 012201 020239 015153 015156 004380 015702 CL25022 2580635 chr2 - 150101637 150152607 1.05 NM_ // NM_ // 001038707 NM_ // NM_ 030913 NM_ // 001079846 NM_ 40 004501 NM_ // NM_ 031844

45 C2orf25 M_ GLG1 // GLG1 // CDC42SE1 SEMA6C CREBBP HNRPU

50 Taybi syndrome)

55 like WDR45L 019613 NM WIPI- box transcription factor 1 HBP1 NM_ chromosome 2 open reading reading open 2 chromosome frame 25 WDR45- HMG- PHD finger protein 3 protein finger PHD PHF3 NM_ CREB binding protein protein binding CREB (Rubinstein- // 1 protein apparatus golgi CDC42 small effector 1 // sema transmembrane domain, cytoplasmic and (TM), domain domain, (semaphorin) 6C REST corepressor 1 RCOR1 NM_ heterogeneous nuclear nuclear heterogeneous (scaffold U ribonucleoprotein A) factor attachment Gene Name Gene Symbol Accession Synonym

279 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3643703 chr16 + 1289451 1317016 1.05 3092276 chr8 + 30059542 30115386 1.05 2945677 chr6 - 24798431 24851423 1.05 3395416 chr11 - 122429309 122438895 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) C35887,1 // P18 // // // P18 C35887,1 UBC9 N155 // KIAA0791 2853768 chr5// CHS1 CHS - 2461999 chr1 37325714 37407016 - 1.05 233878999 234113611 1.05 HSPC112 // Vps55 // Vps55 HSPC112 // my047 DKFZP564G182 // DKFZP564G182 // FLJ12619 Nbla00237 // // dJ30M3.2 XTP12 35 // HSC70 // HSC54 // HSP71 // HSC71 // HSPA10 HSP73 // LAP1 // MGC131511 // MGC29929 // CD16 // NIP71 003345 194260 004298 000081 015344 030939 006597 000570 NM_ // NM_ // 194259 NM_ // NM_ 194261 NM_ // NM_ 153485 NM_ // NM_ 001005736 40 NM_ // NM_ // 153201 NM_

45 UBE21 LEPROTL1 NM_ C6orf62 NM_ HSPA8 // HSPA8 FCGR3B

50 like 1 55 enzyme conjugating nucleoporin 155kDanucleoporin regulator trafficking lysosomal NUP155 LYST ubiquitin- yeast) homolog, E21 (UBC9 leptin receptor overlapping overlapping receptor leptin transcript- chromosome 6 open reading reading open 6 chromosome frame 62 heat shock 70kDa protein 8 // Fc 8 // protein 70kDa shock heat IIIb, affinity low IgG, of fragment (CD16b) receptor Gene Name Gene Symbol Accession Synonym

280 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3600744 chr15 + 70553731 70666726 1.05 3757840 chr17 - 37718873 37794201 1.05 2903343 chr6 + 33044392 33057253 1.05 3176209 chr9 + 81269283 81552230 1.05 3212294 chr9 - 85772377 85785355 1.05 2904877 chr6 + 36103487 36186989 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (sp1) // // (sp1) (continued) 1 // E 1 // ARI // HARI // // HARI ARI HHARI // APRF // FLJ20882 // FLJ20882 // APRF MGC16063 D6S113E // D6S113E // DKFZp686N0336 // FSRG1 FLJ31942 NAT // KIAA9001 // RNF3 RING3 // // ESG // ESG4 // GRG4 BCE- CSBP // FLJ41122 // FLJ41122 CSBP // HNRNPK // TUNP NRF2 // - // NRF2 2588827 chr2 - 177794809 177837753 1.05 35 CSBP2 // // CSBP1 EXIP // // CSPB1 // // PRKM14 Mxi2 // RK // PRKM15 // p38 // SAPK2A p38ALPHA 005744 003150 213662 005104 007005 002140 031263 025160// MIP2 FLJ21016 2458082 chr1 - 222639474 222691338 1.05 006164 001315 139013 NM_ // NM_ // 139276 NM_ NM_ // NM_ // 031262 NM_ NM_ // NM_ 182585 40 NM_ // NM_ // 139012 NM_ // NM_ 139014

45 ARIH1 NM_ STAT3 TLE4 NM_ HNRPK NFE2L2 // NFE2L2 DKFZp451 M21 19 MAPK14 phase phase 50 derived like enhancer of split split of enhancer like

55 protein activated (sp1) homolog, Drosophila) ariadne homolog, ubiquitan- homolog, ariadne E2 binding enzyme conjugating (Drosophila) 1 protein, response factor) response signal transducer and activator activator and transducer signal (acute- 3 transcription of bromodomain containing 2 containing bromodomain BRD2 NM_ transducin- 4 (E heterogeneous nuclear nuclear heterogeneous K ribonucleoprotein WD repeat domain 26 domain repeat WD WDR26 NM_ nuclear factor (erythroid- factor nuclear protein // hypothetical 2 2)-like DKFZp451M2119 kinase 14 kinase mitogen- Gene Name Gene Symbol Accession Synonym

281 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3666146 chr16 + 66855932 66893223 1.05 3896034 chr20 - 4655529 4752291 1.05 3960629 chr22 -3419147 chr12 37202800 + 37232288 1.05 60940328 61086166 1.05 2913983 chr6 + 76367955 76484717 1.05 3908831 chr20 - 47233911 47420063 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 2

30 (continued) DKFZp686K15246 DKFZp686K15246 // LAT- KIAA0245 // // y+LAT- // LAT3 2 DKFZp78101747 // // DKFZp78101747 KIAA0168 // PYST1MKP3 3464860 chr12 - 88223376 88273467 1.05 DKFZp761 H2016 // H2016 DKFZp761 RH70 // P72 // KWA0529 // MGC131982 // MGC149838 // MGC74854 UNPH4 FLJ11355 // FLJ11355 // FLJ11887 // KIAA0389 // SSP1 KIAA0797 SUSP1 35 // FLJ39275 // MGC131926 // PP4052 003983 014737 001946 001429 p300 3946615 chr22 + 39817736 39906025 1.05 006386 006313 015571 021035 NM_ // 001076785 NM_ NM_ 170774 // NM NM_ // NM_ 022652 NM_ // NM_ 030881 40 NM_ // NM_ // 001042471 018530 NM

45 SLC7A6 RASSF2 DDX17 SENP6 NM_ ZNFX1 // GSDML 6) like 50 Asp) box box Asp) type type Ala- Glu-

55 dual specificity phosphatase 6 phosphatase specificity dual DUSP6 p300 protein binding E1A EP300 NM_ solute carrier family 7 (cationic (cationic 7 family carrier solute y+ transporter, acid amino system), member 6 ubiquitin specific peptidase 15 peptidase specific ubiquitin USP15 (RaIGDS/AF- association Ras 2 family domain NM_ DEAD (Asp- polypeptide 17 polypeptide SUMO1 / sentrin specific 6 peptidase zinc finger, NFX1- finger, zinc gasdermin- 1 // containing Gene Name Gene Symbol Accession Synonym

282 EP 2 136 209 A1

5 Fold Change /nM

15 + 359569 372958 1.05 Strand Start Stop

20 chr1_ra ndom Chrom osome Human Genome hg18 Genome Human

25 3945396 chr223538893 + chr14 37431694 + 37459514 1.05 60816958 61087440 1.05 3416036 chr12 +2485433 chr2 52132173 52161417 + 1.05 64604969 64714437 1.05 4041923 3774029 chr17 - 77134363 77214526 1.05 Transcript Transcript ID Cluster 2622469 chr3 + 50101372 50134000 1.05 Human ST Exon 1.0

30 (continued) E2 ISO // HLA- // HLA- ISO 6B // 6B // 1 // GP1 // // GP1 1 HNRPE2 // HNRPE2 // MGC110998 hnRNP- GP- // HSPC018 MGC20069 // MGC26269 // PKC- L MGC5363 // // PRKCL PKCL // nPKC- FLJ20080 // FLJ20080 // FLJ23793 // MGC33965 Nbla10388 ANIA- // DKFZp761A1210 // DKFZp7620195 HCLA- // ISO PCEE // AKIP // AIP SB138 // FLJ20608 FLJ20657 // FLJ20657 // KIAA FLJ23742 1499 //NPL4 35 // // G15 FLJ39876 // LUCA15 // H37 RMB5 005016 004286 006255 017657 030937 017921 005778 NM_ // NM_ 031989 NM_ // 001002243 NM_ // NM_ 203437 40 NM // 001039577 NM_ // NM_ 017900

45 CCNL2 // // CCNL2 AURKAIP1 NPLOC4 NM_

55 (rC) binding protein 2 protein binding (rC) PCBP2 protein kinase C, eta C, kinase protein PRKCH NM_ aftiphilin 1 protein binding GTP GTPBP1 AFTPH NM_ poly cyclin L2 // aurora kinase A kinase // aurora L2 cyclin interacting protein 1 nuclear protein localization 4 localization protein nuclear (S. cerevisiae) homolog RNA binding motif protein 5 RBM5 NM_ Gene Name Gene Symbol Accession Synonym

283 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2418000 chr1 - 71292434 71355820 1.05 3529156 chr14 + 23008821 23048896 1.05 Transcript Transcript ID Cluster 2520291 chr22901913 + chr6 191453802 + 191538513 1.05 30795977 30801165 1.05 Human ST Exon 1.0 2

30 56 // 56 (continued) cl. DKFZp686J1831 DKFZp686J1831 DKFZp686N09117 // // ZIS FLJ41119 // // ZIS2 // ZIS1 ZNF265 C14orf120 // C14orf120 // DKFZP5640092 // NGD // Ipd- LCP5 35 DKFZp686015119 // 10358 FLJ // KIAA0838 // GLS1 MGC117247 // M40 // MGC16435 // OK/SW- TUBB5 TUBB1 005455 015514 014905 178014 033371 033371 932900 932906 945161 945166 NM_ // NM_ 203350 40 XM_ // XM_ // 932898 XM_ // XM_ // 932903 XM_ // XM_ // 941350 XM_ // XM_ // 945163 XM_ 945170 // XM // NM_ // 001042635 NM_

45 ZRANB2 NGDN

50 binding binding

55 zinc finger, RAN- finger, zinc domain containing 2 containing domain tubulin, betatubulin, TUBB binding EIF4E neuroguidin, protein NM_ glutaminase GLS NM_ Gene Name Gene Symbol Accession Synonym

284 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2908474 chr6 + 44319983 44330383 1.05 3419239 chr123396916 + chr11 61146751 - 61280506 1.05 125636504 125644013 1.05 3683050 chr16 - 18719381 18845318 1.05 3385175 chr11 - 85345353 85458481 1.05 3250055 chr10 +3398482 chr11 70380584 - 70414821 1.05 130250320 130291615 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 30 (continued) BETA // BETA 5A 3553607 chr14 + 102743652 102881108 1.05 II/GU // RH- II/GU EIF- D6S182 // D6S182 // FLJ26984 HSP90- HSPC2 // HSP90B HSPCB // KIAA1040 // // KIAA1040 MGC35493 // // MGC17355 DP // MGC3650 SRP- // MGC9571 alpha // Sralpha 61E3.4 // ATX // ATX // // 61E3.4 LIP // KIAA0421 CALM // CLTH // // CLTH CALM LAP 35 DKFZp686F21172 // GURDB // // GUA RH- II/GuA // CHET8 // DKFZp6671205 KIAA0254 001969 007355 015026 003139 015092 007166 004728 014758 NM_ // NM_ 183004 40 NM_ // 001008660 NM_

45 EIF5 HSP90AB1 NM_ SRPR NM_ SMG1 NM_ PICALM DDX21 NM_

50 Asp) box box Asp) Ala- Glu- related kinase kinase related

55 ’docking protein’) 1 kinase- 3- eukaryotic translationinitiation 5 factor signal recognition particle particle recognition signal ( receptor alpha 90kDa protein shock heat 1 B member class (cytosolic), MON2 homolog (S. cerevisiae) (S. homolog MON2 MON2 NM_ PI- SMG- sorting nexin 19 nexin sorting binding phosphatidylinositol protein assembly clathrin SNX19 NM_ DEAD (Asp- polypeptide 21 polypeptide Gene Name Gene Symbol Accession Synonym

285 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3159946 chr9 + 1968220 2253060 1.05 3730899 chr17 + 59204975 59250510 1.05 3056044 chr7 - 72492710 72574552 1.05 3735107 chr17 + 71174801 71215729 1.05 3067592 chr7 - 107880325 107956012 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) (GAMMA) BAF190 // BRM // BRM // // BAF190 // FLJ36757 SNF2 // MGC74511 // SNF2L2 // // // SWI2 SNF2LA // // hBRM Sth1p hSNF2a FLJ43179 // RHELP // RHELP FLJ43179 RNAHP // // SF3b125 WBSCR10 // WBSCR10 WSTF // WBSCR9 DKFZp586L2022 // // DKFZp586L2022 HTRG // HCNGP // // // BSF3 HTRP CLC // // CISS2 NR6 // NNT1 MP100 // PSA // MP100 3724698 chr17 + 42955347 43057168 1.05 35 IPLA2 // - // IPLA2G IPLA2-2 // 003070 007372 003590 2601544 chr2 - 225025520 225158348 1.05 023005 013260 006310 006187 // MGC133260 3432467 chr12 + 111860550 111895663 1.05 015723 927062 927062 NM_ // NM_ 139045 NM_ // NM_ 203499 NM_ // NM_ 032408 NM_ // NM_ 013246 XM_ // 001128588 NM_ 40 XM_ // XM_ // 938392 NM_

45 SMARCA2 DDX42 BAZ1B SAP30BP // SAP30BP CLCF1 NPEPPS OAS3 NM_ PNPLA10P // PNPLA8

50 like like Asp) box box Asp) Ala- like cytokine Glu-

55 like phospholipase phospholipase like oligoadenylate synthetase synthetase oligoadenylate 5’- ’- SWI/SNF related, matrix matrix related, SWI/SNF dependent actin associated, of chromatin, regulator 2 member a, subfamily DEAD (Asp- polypeptide 42 polypeptide cullin 3cullin CUL3 NM_ bromodomain adjacent to zinc 1B domain, finger SAP30 binding protein // protein binding SAP30 cardiotrophin- 1 factor aminopeptidase puromycin puromycin aminopeptidase sensitive 3, 100kDa 3, 2 patatin- 10 containing domain patatin- // pseudogene domain phospholipase 8 containing Gene Name Gene Symbol Accession Synonym

286 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2404158 chr1 - 30977913 31095913 1.05 3630912 chr15 -3226097 chr9 66857944 66900452 - 1.05 129615329 129660473 1.05 2618640 chr3 + 40473807 40485068 1.05 2548970 chr2 - 38824253 38832154 1.05 3334224 chr11 + 63709341 63728586 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 SSP- SSP- 7 // CTG- 7 // (continued) ISL- MGC125860 // MGC125860 MGC125861 PP32R1 // C15orf1 // C15orf1 PP32R1 LANP // // IIPP2A // // MAPM // MGC119787 // MGC150373 PHAPI // // PHAP1 PP32 // END CD105 // // HHT1 FLJ41744 //ORW ORW1 CAG- // L14 // B33 RL14 // MGC88594 bcm1298 // hRL14 // 9G8 // AAG3 // AAG3 // 9G8 // RBM37 // HSSG1 // ZCCHC20 ZCRB2 35 IEF- // HOP STI1L // P60 // 3521 006762 012403 000118 003973 006819 017790 NM_ // NM_ 006305 017789 // 017789 XR- NM_ // 001034996 NM_ // XR_ 40 NM_ 001031684

45 LAPTM5 NM_ ENG NM_ ANP32C // ANP32A RPL14 // RPL14L SFRS7 STIP1 NM_ rich) rich) serine- 50 Weber like organizing Rendu- phosphoprotein phosphoprotein rich) nuclear nuclear rich)

55 induced- endoglin (Osler- endoglin lysosomal associated membrane multispanning 5 protein syndrome 1) phosphoprotein 32 family, family, 32 phosphoprotein (leucine- // acidic C member acidic (leucine- acidic 32 phosphoprotein nuclear A member family, ribosomal protein L14 // L14 protein ribosomal L14- protein ribosomal rich 7, rich 35kDa splicing factor, arginine/ factor, splicing stress- 1 (Hsp70/Hsp90- protein) Gene Name Gene Symbol Accession Synonym

287 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2884658 chr5 - 159761226 159778959 1.05 3545466 chr14 + 76993989 77005560 1.05 2589929 chr2 - 179644888 180002479 1.05 3604287 chr15 + 79262148 79392377 1.05 3845581 chr19 - 1827984 1836490 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 // 16 16 (continued) COP 2697792 chr3 - 140555482 140591192 1.05 FLJ22344 2867443 chr5 - 94066156 94646035 1.05 9G8 // MGC9280 // MGC9280 // 9G8 hSlu7 AHA1 //C14 or f3 // f3 or //C14 AHA1 p38 DKFZp43400515 // // DKFZp43400515 SOLO FLJ16806 // FLJ16806 // FLJ42735 // FLJ44234 IL- // HsT19289 prIL- // LCF 35 // C19orf27 C1orf47 MGC5244 // 024717 006425 004766 beta- 001997 RPS30 // FAU1 3377463 chr11 - 64644697 64646234 1.05 178123 004513 031213 039721 039721 012111 NM_ // 001002796 NM_ NM_ // NM_ 172217 40 XM_ // XM_ // 933830 NM_ // 001080422 NM_

45 MCTP1 AHSA1 M_ SLU7 NM_ FAU NM_ COPB2 NM_ IL16 FAM108A2 // FAM108A2 FAM108A1

50 MuSV) MuSV) Reilly murine murine Reilly

55 Biskis- multiple C2 domains, domains, C2 multiple transmembrane 1 AHA1, activator of heat shock shock heat of activator AHA1, homolog ATPase protein 90kDa 1 (yeast) SLU7 splicing factor homolog homolog factor splicing SLU7 cerevisiae) (S. ubiquitously expressed (fox (fox expressed ubiquitously derived); ribosomalprotein S30 coatomer protein complex, complex, protein coatomer prime) (beta 2 beta subunit Finkel- (FBR- virus sarcoma SEC14 and spectrin domains 1 domains spectrin and SEC14 SESTD1 NM_ interleukin 16 (lymphocyte factor) chemoattractant family with sequence similarity similarity sequence with family with // family A2 member 108, 108, similarity sequence member A1 Gene Name Gene Symbol Accession Synonym

288 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2988536 chr7 + 5196360 5239975 1.05 3214668 chr9 -3551677 chr14 94012330 + 94096287 1.05 99750383 99818868 1.05 2599955 chr2 - 219781799 219802587 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 2

30 E1 // 50 // // 50 (continued) 1 Atg21 // CGI- Atg21 // DKFZP434J154 DKFZp686P02188 // FLJ12979 // // FLJ14217 // WIPI- FLJ42984 FLJ20736 // IARS1 // IARS1 FLJ20736 // PRO0785 ILRS // NF- // DELTA YIN- UCRBP // YANG- APG9L1 // APG9L1 // ABC // MGD3208 ABC14 // // EST45597 // FLJ22414 // // PRP MTABC3 umat 35 FLJ30780 3767053 chr17 - 60176255 60263758 1.05 015610 002161 003403 024085 015622 015622 NM_ // 001033518 NM_ // 001033519 NM_ // 001033520 NM_ // NM_ 016003 NM_ // NM_ 013417 NM_ NM_ // 001077198 NM_ // NM_ 005689 40 XR_ // XR_ 016048

45 WIP12 UBE2Z 023079 NM // FLJ13855 3725481 chr17 + 44340808 44361870 1.05 ATG9A // ATG9A ABCB6

50 tRNA synthetase LARS 55 enzyme conjugating binding cassette,sub- LIM domain binding 1 binding domain LIM YY1 transcription factor LDB1 YY1 domain, repeat WD 003893 NM 2 interacting phosphoinositide NLI // CUM2 NM_ 3304215 chr10 - 103830793 103883389 1.05 isoleucyl- ubiquitin- E2Z (putative) MGC40489 protein hypothetical MGC40489 9 related autophagy ATG9 // cerevisiae) A (S. homolog ATP- family B (MDR/TAP), member 6 member B (MDR/TAP), family Gene Name Gene Symbol Accession Synonym

289 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3579114 chr14 - 98705377 98931503 1.05 3261492 chr10 + 103901962 103913597 1.05 2391532 chr1 - 1314609 1324575 1.05 3890555 chr20 + 55359493 55386992 1.05 2883440 chr5 - 156755122 156935351 1.05 2975680 chr6 - 136619703 136652847 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) ISO // HLA- // HLA- ISO 6B // 6B // 2 // CTIP2 // CTIP2 2 // CTIP- hRIT1- // RIT1 KIAA0035 // // KIAA0035 // NOPP130 // NOPP140 P130 // NS5ATP13 ANIA- // DKFZp761A1210 // DKFZp7620195 HCLA- // ISO PCEE // AKIP // AIP SB138 // FLJ20608 FLJ30608 // FLJ30608 // MGC117333 // MGC126076 // MGC126077 // MRNP41 // MIG14 // dJ481 Mnrp41 dJ800J21.1 // F12.3 FKSG34 // // FKSG34 MADDAM // 35 // MAA0164 // BTF bK211L9.1 022898 004741 030937 003610 023038 NM_ // NM_ 138576 NM_ // 001039577 NM_ // NM_ 017900 NM_ NM_ // 001015885 NM_ NM_ // NM_ 033274 40 NM_ // 001077440 NM_ // 001077441 014739 NM

45 BCL11B NOLC1 NM_ CCNL2 // // CCNL2 AURKAIP1 RAE1 ADAM19 BCLAF1

50 body body lymphoma 11B (zinc (zinc 11B lymphoma 55 associated transcription transcription associated cell CLL/ B- protein) finger nucleolar and coiled- and nucleolar phosphoprotein 1 phosphoprotein cyclin L2 // aurora kinase A kinase // aurora L2 cyclin interacting protein 1 RAE1 RNA export 1 homolog (S. pombe) ADAM metallopeptidase metallopeptidase ADAM beta) (meltrin 19 domain BCL2- 1 factor Gene Name Gene Symbol Accession Synonym

290 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3740304 chr17 -2765590 chr4 1367883 1412932 - 1.05 35626248 35922356 1.05 3829575 chr19 + 39355192 39416345 1.05 2655650 chr3 + 185499199 185509504 1.05 3289031 chr10 - 51180787 51293382 1.05 3544905 chr14 + 75688015 75800924 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) MGC99649 // MGC99649 VIB1A // // PITPN // MMI- FLJ23903 NMI // // MMIb beta // myr2 FLJ13675 // ARAP2 // FLJ44916 // C19 or f 13 // f 13 or C19 // DKFZP434D1335 RAP55 A // FAM61 MGC14274 // P97 // // P97 // MGC14274 TRAP2 // S2 MGC22767 // MGC22767 // TIM23 PRO11197 TIMM23B // 35 // FLJ10033 // FLJ20689 MGC61896 006224 033375 015230 015578 002808 006327 017926 002811 S12 // P40 // MOV34 3668617 chr16 + 72888182 72901528 1.05 NM_ // NM_ // 001080779 NM_ // 001080950 NM_ NM_ // NM_ 139182 XM_ // 001133798 NM_ 40 NM_ // NM_ 017972

45 PITPNA // PITPNA MYO1C LSM14A NM_ PSMD2 NM_ TIMM23 C14orf118 PSMD7 NM_

55 centaurin, delta 1 delta centaurin, CENTD1 phosphatidylinositol transfer transfer phosphatidylinositol IC myosin // alpha protein, LSM14A, SCD6 homolog A (S. SCD6 homolog LSM14A, cerevisiae) proteasome (prosome, (prosome, proteasome non- subunit, 26S macropain) ATPase, 2 ATPase, translocase of inner inner of translocase mitochondrial membrane 23 (yeast) homolog chromosome 14 open reading frame 118 proteasome (prosome, (prosome, proteasome non- subunit, 26S macropain) ATPase, 7 (Mov34 homology) (Mov34 7 ATPase, Gene Name Gene Symbol Accession Synonym

291 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2921086 chr6 + 110606544 110682171 1.04 3375340 chr11 - 60926704 60954030 1.04 3352948 chr113565739 + chr14 - 120828130 121077997 1.04 54902008 54948457 1.04 3373845 chr11 - 56931008 56951629 1.04 4009238 chrX - 53417797 53466400 1.05 Transcript Transcript ID Cluster Human ST Exon 1.0 1 //

30 // 13 (continued) 1 EHB3 // FLJ10564 // FLJ10564 // EHB3 // MGC102802 PRPF17 // PRP17 FLJ39024 // FLJ39024 MGC9315 LR11 // LRP9 // // LRP9 LR11 SorLA- // SORLA gp250 // MGC126291 MGC126292 DKFZp762A227// DKFZp762A227// FOAP- // EEG1 // PRO1659 SEEEG- FLJ22858 3601741 chr15 + 72677906 72719105 1.04 35 DKFZp686L19178 // DXS423E // // KIAA0178 // MGC138332 // SB1.8//SMC1 // SMC1L1 // SMC1alpha 015891 007190// P125 MSTP053 3267455 chr10 + 121642213 121691984 1.04 024811 003105 014924 006725 TP120 3332663 chr11 + 60495619 60544422 1.04 014096 199329 004148NINJURIN // NIN1 001292 3215146 chr9 - 94923613 94939639 1.04 006306 NM_ NM_ // NM_ // 017611 NM_ 40 NM_ // NM_ 003992

45 CDC40 NM_ FLJ12529 NM_ SORL1 // SORL1 C11orf32 SLC43A3 SMC1A NM_ (DLR 50 containing

55 related receptor, L like kinase 3 kinase like CLK3 mRNA cleavage factor 1, 59 factor cleavage mRNA cell division cycle 40 homolog homolog 40 cycle division cell cerevislae) (S. SEC23 interacting protein interacting SEC23 SEC231P NM_ KIAA0831CD6 molecule KIAA0831 CD6 NM_ NM_ pre- subunit kDa class) A repeats- class) ninjurin 1ninjurin sortilin- NINJ1 NM_ CDC- solute carrier family 43, member member 43, family carrier solute 3 structural maintenance of maintenance structural chromosomesA 1 Gene Name Gene Symbol Accession Synonym

292 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3656904 chr16 + 31093395 31111003 1.04 3959631 chr22 - 35236857 35255429 1.04 3894228 chr20 - 402069 472534 1.04 2761285 chr4 - 13179462 13207890 1.04 3902764 chr203667281 - chr16 + 30498759 30636537 69115212 1.04 69169072 1.04 Transcript Transcript ID Cluster 2844203 chr5 + 179058077 179091243 1.04 Human ST Exon 1.0

30 zeta // zeta CHOP (continued) 362G6.1 // LKAP // 362G6.1 3681956 chr16 - 15595757 15654441 1.04 CHOP // FUS- // CHOP // FUS1 // CHOP TLS/ // TLS MGC126526 // MGC126526 // eIF3- MGCI7258 // eIF3- p66 eIF3d CK2A1 // CKII // CKII // // CK2A1 // - alpha CKH FLJ33215 // FLJ33215 KIAA1327 DKFZP566G1424 // DKFZP566G1424 dJ1184F4.2 // RSE1 KIAA0017 SF3b130 // SAP130 STAF130 // 35 // CNX // FLJ26570 // P90 IP90 012426 004960 014647 A- 003753 001895 148894 080616 001746 002207 019096 MGC74725 2954771 chr6 - 43681031 43704877 1.04 NM_ // 001010850 NM_ NM_ // NM_ 11 177559 // 177560 NM NR_ 40 NM // 001024649 NM_

45 FUS EIF3S7 NM_ CSNK2A1 II II CSNK2A1 CSNK2A1P SF3B3FAM44A N M_ NM_ C20orf112 NM_

50 in 16) (12:

55 KIAA0430 KIAA0430 NM_ GTP binding protein 2 protein binding GTP t in (involved fusion GTPBP2 NM. malignant liposarcoma) malignant eukaryotic translationinitiation zeta, 7 subunit 3, factor 66/67kDa casein kinase 2, alpha 1 1 2, alpha kinase casein 2, kinase casein // polypeptide polypeptide 1 alpha pseudogene splicing factor 3b, subunit 3, 3, subunit 3b, factor splicing 130kDa similarity sequence with family A member 44, calnexinchromosome 20 open reading frame 112 CANX Gene Name Gene Symbol Accession Synonym

293 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2866045 chr5 - 87526693 87600565 1.04 Transcript Transcript ID Cluster 3512874 chr13 - 45595067 45684007 1.04 Human ST Exon 1.0

30 (continued) EWS 3941907 chr22 + 27994201 28026501 1.04 FLB3342 // // 4 MGC3321 // // CD41 PR01313 // GP2B B // CD41 // // GTA GPllb HPA3 KIAA1565 3564071 chr14 - 50256234 50403020 1.04 - 3572041 chr14 - 74189599 74249655 1.04 35 // CP64 DKFZp781A23186 // FLJ25423 // // FLJ26114 // L- FLJ39956 LC64P // PLASTIN PLS2 // 005243 153354 016350 182944 182946 014957 K1AA0870 3118651 chr8 + 142207943 142289494 1.04 002298 NM_ // NM_ 013986 NM_ // NM_ 000419 NM_ // NM_ // 020921 NM_ // NM_ // 182945 NM_ 40 NM_ 001039479

45 EWSR1 TMEM161B // // TMEM161B ITGA2B NIN DENND3 NM_ LCP1 NM_

55 MADD domain domain MADD plastin) Ewing sarcoma breakpoint breakpoint sarcoma Ewing 1 region transmembrane protein 161 B // (platelet 2b alpha integrin, IIb/IIa of IIb glycoprotein complex, antigen CD41 ) ninein (GSK3B interacting interacting (GSK3B ninein protein) K1AA0317 KIAA0317 lymphocyte cytosolic protein 1 protein cytosolic lymphocyte (L- DENN/ 3 containing Gene Name Gene Symbol Accession Synonym

294 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2330687 chr1 + 37712740 37722550 1.04 2530599 chr2 + 228045122 228134167 1.04 2728448 chr4 + 57539163 57592513 1.04 3262433 chr10 + 105716666 105778975 1.04 3463571 chr12 - 78690959 78853356 1.04 2573641 chr2 - 121811825 122169321 1.04 3470253 chr12 - 107440140 107479296 1.04 Transcript Transcript ID Cluster 2772017 chr4 - 68858700 68934802 1.04 Human ST Exon 1.0

30 (nrb) (continued) B FLJ23231 // MCPIP // MCPIP FLJ23231 // 423B22.1 RP3- // MG01 16938 II 16938 MG01 RAB // MGC116940 II RIP POL2RB // RPB2 II RPB2 II // POL2RB hRPB140 II hsRPB2 KIAA0204 // // KIAA0204 // MGC133067 STK2 // bA16H23.1 se20-9 // MBS // MGC133042 MGC133042 // MBS // DKFZp686D1968 // // DKFZp686D1968 // DKFZp686H2039 // FLJ33821 // FLJ41222 // KIAA0622 // MAST1 KIAA0156 // // KIAA0156 // MGC138188 // RP11-13G14 p110 // TIP110 35 // YT521 KIAA1966 YT521- // 025079 000938 014720 002480 015282 003489 RIP140 3925639 chr21 - 15255125 15359182 1.04 014706 133370 941338 941338 XM_ // NM_ 004504

40 NM_ // 001031732 NM_

45 ZC3H12A NM_ POLR2B NM_ SLK NM_ PPP1R12A NM_ CLASP1 NM_ SART3 NM_

50 like kinase kinase like type type

55 1 Rev binding protein binding Rev 1 HRB zinc CCCH- finger 12A containing HIV- polymerase (RNA) II (DNA (RNA) II polymerase B, 140kDa polypeptide directed) subunit 12A STE20- 12A subunit (yeast) nuclear interacting protein 1 protein interacting nuclear NRIP1 NM_ receptor protein phosphatase 1, 1, phosphatase protein receptor (inhibitor) regulatory cytoplasmic linker associated associated linker cytoplasmic 1 protein YTH domain containing 1 YTHDC1 carcinoma cell squamous 3 T cells by recognized antigen Gene Name Gene Symbol Accession Synonym

295 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3405531 chr12 + 12856462 12874176 1.04 3326183 chr11 + 34009711 34081946 1.04 3161566 chr9 + 6747651 7165647 1.04 3863021 chr19 - 46499343 46551636 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) DBP // DKFZp5640176 // DKFZp5640176 E4- // FLJ30012 // HQ0256 // MSTP162 // DKFZP434F0318 FLJ25138 GP1P137 // M11S1 M11S1 // GP1P137 p137GPI // FLJ25949 // FLJ25949 GASC1 // JHDM3C // KIAA0780 // bA146B14.1 - 2678090 chr3 - 57532172 57558635 1.04 35 // DPD1 // CED TGFB 016355 030817 005898 022152 RECS1 // PP1201 2599371 chr2 - 218847185 218865515 1.04 002657 FLJ23283 015061 3902682 chr20 - 30243975 30259284 1.04 001660 000660 NM_ // NM_ // 201224 NM_ NM_ // NM_ 203364 40 XM_ // 001132763 NM_

45 DDX47 // // DDX47 APOLD1 GPIAPI TMBIM1 NM_ PLAGL2 NM_ TGF81 NM_

50 Asp) box box Asp) Ala- Glu-

55 ribosylation factor 4factor ribosylation ARF4 anchored membrane membrane anchored DEAD (Asp- polypeptide 47 // apolipoprotein 47 // apolipoprotein polypeptide 1 containing domain L GPI- 1 protein transmembrane BAX inhibitor BAX inhibitor transmembrane 1 containing motif jumonji domain containing 2C containing domain jumonji JMJD2C NM_ pleiomorphic adenoma gene- adenoma pleiomorphic 2 like ADP- transforming growth factor, beta beta factor, growth transforming 1 Gene Name Gene Symbol Accession Synonym

296 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3655665 chr16 + 29724956 29729977 1.04 2901620 chr6 + 30565243 30620086 1.04 3351675 chrl1 + 118259777 118272180 1.04 2796484 chr4 - 185782536 185807608 1.04 2417174 chr1 -2458289 67646101 chr1 67669020 1.04 - 223655840 223683230 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0 2

30 // 2 1 // 1 // (continued) 1 II OBP- 1 1 1 // SAF- 1 // 6.2 // MHC 6.2 55 // CHD31P // 55 PUR1 // Pur- PUR1 SAF- // // ZNF801 ZF87 KID // // Zif87 OBP II // KNSL4 OBP- DKFZp686P19218 DKFZp686P19218 // EA2.1 // EA1.2 // HLA- CD185 // CXCR5 // // CXCR5 // CD185 // MOR15 MGC117347 CPP32 // CPP32B CPP32 SCA- 35 CGI- DKFZp564M2423 // // FLJ90489 // PAI- // HABP4L PAIRSP1 // RBP1 // DHCR14B // LMN2R PHA // MGC9041 002383 002350// JTK8 FLJ26625 3098977 chr8 + 56954505 57087291 1.04 001716 004346 015640 020198 MSTP041 // GK001 002296 3766334 chr17 - 59176353 59204726 1.04 005516 NM NM // 001042539 NM_ // NM_ 007317 NM_ // NM_ 032966 NM_ // NM_ 032991 40 NM_ // 001018067 NM_ // 001018068 NM_ // 001018069 NM_ NM_ // NM_ 194442

45 ENM- MAZ // KIF22 MAZ LYN NM_ HLA- BLR1 CASP3 SERBP1

50 related related C motif) X- binding

55 coil domain containing 47 CCDC47 NM_ 1 Yamaguchi sarcoma sarcoma Yamaguchi 1 associated zinc finger finger zinc associated yes- MYC- (purine- protein kinesin // factor) transcription 22 member family v- viral related oncogene homolog oncogene related viral major histocompatibility E I, class complex, Burkitt lymphoma receptor 1, 1, receptor lymphoma Burkitt protein binding GTP (C- (chemokine 5) receptor coiled- apoptosis- 3, caspase cysteine peptidase cysteine lamin B receptor B lamin LBR SERPINE1 SERPINE1 mRNA binding 1 protein Gene Name Gene Symbol Accession Synonym

297 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3509910 chr13 - 36480880 36556254 1.04 3099750 chr8 + 59605208 59658960 1.04 2626167 chr3 + 58293657 58386884 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 9 // ST1 // // ST1 9 C 13 // C 13orF19 // 13orF19 C // 13 C // P381P // FP757 - // bA421P11.4 MDA- TACIP18 // SYCL 35 // FLJ20335 MONaKA 017569 033133 CNP1 3721548 chr17 + 37372285 37383765 1.04 005625 015939 MGC5029 3896524 chr20 - 5865881 5879370 1.04 004973 JMJ 2896177 chr6 + 15261674 15630231 1.04 017771 003922p619 // p532 014741 FLJ20698 3628650 chr15 3329404 - chr11 61687879 + 61913158 1.04 46595671 46652934 1.04 173552 MGC33365 2646327 chr3 + 145173603 145669744 1.04 NM_ // 001014286 NM_ // XM_ 293352 NM_ // 001007067 NM_ // 001007068 NM_ // 001007069 NM_ // 001007070 NM_ 40 NM_

45 09 NM_ FAM48A // // FAM48A FAM48B2 CNP NM_ SDCBP JARID2 // C20orf120 PXK NM_ HERC1 NM_ C3orf58 NM_ AP

55 cyclic nucleotide 3’ nucleotide cyclic 09 protein 09 CGI- 3’- ’, family with sequence similarity similarity sequence with family with A // family member 48, member 48, similarity sequence B2 2 phosphodiesterase syndecan binding protein protein binding syndecan (syntenin) CGI- jumonji, AT rich interactive interactive rich AT jumonji, 2 domain KIAA0652 serine/ containing PX domain KlAA0652 NM_ threonine kinase threonine hect (homologous to the E6- the to (homologous hect terminus) carboxyl (UBE3A) and RCC1domain (CHC1)-like (RLD) 1 domain chromosome 3 open reading reading open 3 chromosome frame 58 Gene Name Gene Symbol Accession Synonym

298 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3284188 chr10 - 33211051 33321367 1.04 3280902 chr10 - 22078144 22332877 1.04 3510858 chr13 - 40027817 40162098 1.04 2435044 chr1 - 149641830 149753035 1.04 2771718 chr4 - 68130308 68249472 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0

30 14 3223872 chr9 - 122980236 123025093 1.04 (continued) CD29 // FNRB // // CD29 // // MDF2 GPIIA VLAB // MSK12 - 3627363 chr15 - 58500956 58558626 1.04 DNAJL1 // ERdj1 // // ERdj1 DNAJL1 // MGC HTJ1 131954 FKH1 // FKHR // // FKH1 FOXO1 KIAA046 // KIAA046 // MGC71543 ZNF635 // SUHW5 35 // FLJ10808 FLJ23367 002211 033667 033669 024611 022365 018683 RNF114 3888474 chr20 + 47986321 48003818 1.04 002015 016322 FBP // RAB- 015100 207171 005827 UGTREL1 3761959 chr17 - 45133304 45141355 1.04 018227 NM_ // NM_ // 033666 NM_ // NM_ // 033668 NM_ // NM_ 133376 NM_ // 001018089 NM_ 40 NM_ // NM_ // 145796 NM_

45 ITGB1 DNAJC1 NM_ ZNF313 NM_ FOX01A NM_ POGZ SLC35B1 NM_ UBE1L2 NM_

55 El- enzyme activating NMDA receptor regulated 2 regulated receptor NMDA NARG2 integrin, beta 1 (fibronectin (fibronectin 1 beta integrin, polypeptide, beta receptor, MDF2, includes CD29 antigen MSK12) DnaJ (Hsp40) homolog, 1 member C, subfamily RAB14, member RAS family protein finger zinc oncogene RAB14313 NM_ forkhead box 01 A 01 box forkhead (rhabdomyosarcoma) pogo transposable element with with element transposable pogo domain ZNF solute carrier family 35, member member 35, family carrier solute B1 ubiquitin- 2 like Gene Name Gene Symbol Accession Synonym

299 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3815165 chr19 + 747768 763505 1.04 3903708 chr20 - 33053899 33144297 1.04 2594497 chr2 - 201425997 201437659 1.04 3190558 chr9 + 130354704 130435758 1.04 2908052 chr6 + 43592769 43605071 1.04 2937984 chr6 + 170705200 170723945 1.04 3734760 chr17 + 70769374 70774626 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0

30 // S7 (continued) II- S // MRP- 1 // PTB- T // PTB- T 1 // S7 // S7 HNRNPI // HNRPI HNRNPI // HNRPI // // MGC10830 PTB // // MGC8461 PTB- // PTB3 // PTB2 pPTB // PTB4 C20orf188 // C20orf188 // TRRP4AP CLK // CLK/STY // // // CLK/STY CLK STY (ALPHA) // SPECTRIN FLJ44613 RPA39 // RPA40 // RPA40 // RPA39 RPAC1 // RPA5 GTF2D // GTF2D1 // // GTF2D1 GTF2D // 117320 MGC // MGC126054 // MGC126055 TFIID // SCA17 35 MRP- RP- 002819 031991 015638 001101 PS1TP5BP1 3036924 chr7 - 5533433 5537011 1.04 002710 PPP1G 004071 3471374 chr12 - 109642007 109665131 1.04 003127 004875 003194 015971 NM_ // NM_ // 031990 NM_ // NM_ 175847 NM_ // NM_ 199368 NM_ NM_ // 001024646 NM_ 40 NM_ // NM_ 203290

45 PTBP1 TRPC4AP PPP1 CCPPP1 NM_ SPTAN1 NM_ POLRIC MRPS7 NM_

50 fodrin)

55 like kinase 1 kinase like CLK1 actin, betaactin, ACTB NM_ polypyrimidine tract binding binding tract polypyrimidine 1 protein transient receptor potential C, subfamily channel, cation protein 4 associated member CDC- protein phosphatase 1, catalytic catalytic 1, phosphatase protein isoform gamma subunit, spectrin, alpha, non- alpha, spectrin, erythrocytic 1 (alpha- polymerase (RNA) I polypeptide (RNA) I polypeptide polymerase C, 30kDa TATA box binding protein binding box TATA TBP NM_ mitochondrial ribosomal protein protein ribosomal mitochondrial 57 Gene Name Gene Symbol Accession Synonym

300 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2550790 chr2 - 43961504 44085128 1.04 2656738 chr3 + 187961636 187990742 1.04 2873168 chr5 -3593652 chr15 122642038 + 122832582 1.04 3377044 48503634 chr11 48580565 - 1.04 64287827 64302817 1.04 3656555 chr16 + 30681120 30695182 1.04 2963784 chr6 - 88441297 88476721 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) 23970 // 010 // DDX2B // DDX2B // 010 CLONE- GP130// LRP130 // LSFC BM- F ELF4 // EIF4A DKFZp688I06246 // DKFZp688I06246 // FLJ36090 FLJ38327 // FLJ34456 // HumORF8 // KIAA0055 // MGC129718 UBPY // // ZFMI 5636 D11 ZNF162 BRE1B // BRE1B // DKFZp686K191 // KIAA0661 // MGC13051 STARING // RBP95 35 // FLJ10342 dJ486L4.2 133259 152832 MTVR1 3335338 chr11 + 65096490 65098230 1.04 53223 005154 004630 201997 014771 018064

40 NM_ // NM_ // 2019961 NM_ // NM_ 201998

45 LRPPRC NM_ EIF4A2 NM967 FAM89B NM_ CCDC100 NM_ C6orf166 NM_

50 motif

55 rich PPR- rich coil domain containing leucine- containing eukaryotic translationinitiation 2 isoform 4A, factor ubiquitin specific peptidase 8 peptidase specific ubiquitin USP8 NM_ splicingfactors 1 similarity sequence with family B member 89, SF1 coiled- 100 ring finger protein 40 protein finger ring RNF40 NM_ chromosome 6 open reading reading open 6 chromosome frame 166 Gene Name Gene Symbol Accession Synonym

301 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2790570 chr4 - 155675613 155691014 1.04 3255402 chr10 + 86020629 86268247 1.04 3811497 chr18 - 59207407 59240734 1.04 3923354 chr21 + 44105141 44245644 1.04 3838185 chr19 + 54280358 54304714 1.04 2712632 chr3 - 197238405 197334433 1.04 3442054 chr12 - 6549521 6587067 1.04 3377789 chr11 - 65176856 65204491 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) GAMMAL // // GAMMAL 2b // Mi2- 2b MGC110980 // MGC110980 PRL1 FLJ14262 // FLJ14262 // FLJ25809 // Gcap14 bA486022.1 MIG1 // SKD1 // // SKD1 MIG1 VPS4-2 LPAAT- MGC4604 RNPU1Z // RPU1 // RPU1 // // RNPU1Z // // UIAP U170K U1RNP CD71 // TFR TFR1 CD71 TRFR // DKFZp688E06161 DKFZp688E06161 // Mf- 35 // MGC131774 NFKB3 002669 004383 MGC117393 3801840 chr15 + 72841734 72882558 1.04 018999 004869 020132 003089 181717 - 3415193 chr12 + 50686988 50695938 1.04 003234 001273 021975 NM_ // 001037553 NM_ 40 NM_ // 001009820 NM_

45 PLRG1 NM_ VPS4B NM_ AGPAT3 SNRP70 GRASP NM_ CHD4 NM_ RELA NM_

50 celts 3. p65 p65 3. celts phosphate O- phosphate 3-

55 acylglycercl- src tyrosine kinase CSK NM_ rel reticuloendotheliosis viral viral reticuloendotheliosis rel pleiotropic regulator 1 (PRL1 1 (PRL1 regulator pleiotropic Arabidopsis) homolog, c- KIAA1128 KIAA1128 NM_ vacuolar protein sorting 4 sorting protein vacuolar cerevisiae) B (S. homolog 1- 3 acyltransferase small nuclear ribonucleoprotein ribonucleoprotein nuclear small 70kDa polypeptide (RNP antigen) GRP1 (general receptor for for receptor GRP1 (general phosphoinositides protein scaffold 1)-associated transferrin receptor (p90, CD71) (p90, receptor transferrin TFRC NM_ chromodomain helicase DNA DNA helicase chromodomain 4 protein binding v- nuclear A, homolog oncogene factorkappa of lightpolypeptide B- in enhancer gene (avian) Gene Name Gene Symbol Accession Synonym

302 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3070658 chr7 - 122968075 122985216 1.04 2357961 chr1 + 148126062 148138968 1.04 3655920 chr16 + 29968869 29991009 1.04 3836266 chr19 + 50624036 50671180 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0 B // B //

30 1 2760371 chr4 - 9685076 9772600 1.04 (continued) 143 // 143 B13 // 01-13KD- // DKFZp781K1356 // NUFM FLJ12147 // UOOR13 ARAP1 // KIAA0782 // ARAP1 3381241 chr11 - 72073021 72141062 1.04 CGI- // MGC75015 RP11-196G18.18 ALDA // MGC10942 MGC10942 // ALDA // MGC17716 // KIAA1694 3670772 chr16 + 80030441 80323852 1.04 DKFZp686C0818 // // DKFZp686C0818 GOS3 GOS3 // // GOSB // 35 NORI- // AIP1 018321 // FLJ11100 BRIX 2806231 chr5 + 34951248 34962845 1.04 005000 133368 KIAA1972 3662612 chr16 + 55777703 55831882 1.04 015242 016074 000034 184043 030629 006732 005112 NM_ // 001040118 NM_ // NM_ 139181 NM_ // NM_ // 184041 NM_ NM_ // NM_ 198390 40 NM_ // NM_ 017491

45 NDUFA5 NM_ RSPRY1 NM_ ALDOA FOSB NM_

55 inducing protein inducing CMIP Maf- brix domain containing 2 containing domain brix BXDC2 NM_ centaurin, delta 2 delta centaurin, CENTD2 NADH dehydrogenase dehydrogenase NADH alpha 1 (ubiquinone) 13kDa 5, subcomplex, ring finger and SPRY domain domain SPRY and finger ring 1 containing bolA homolog 1 (E. coli) BOLA1 NM_ bisphosphate aldolase A, fructose- A, aldolase c- WD repeat domain 1 domain repeat WD WDRI FBJ murine osteosarcoma viral viral osteosarcoma FBJ murine B homolog oncogene Gene Name Gene Symbol Accession Synonym

303 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 2394699 chr1 - 6443807 6448816 1.04 3482219 chr13 + 24773258 24822202 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0 1 3715109 chr17 + 22644482 22684326 1.04 30 (continued) LR // LR 3 // DDR3 // // DDR3 3 SWIP1 // WSB- SWIP1 35 APO- // // LARD DR3 // TR3 // TNFRSF12 // WSL- 1 // TRAMP WSL- RP4- // KIAA0720 650H14.3 // KIAA0410 PRO2463 015626 004556 IKBE 030912 RNF27 // GERP 3261820 2955076 ehr10 chr6 + - 104384137 104419190 44333884 1.04 44341478 1.04 003790 148966 148970 001 020631 014089 NM_ // NM_ 134265 40 NM_ // 001039664 NM_ // NM_ // 148965 NM_ // NM_ // 148967 NM_ // NM_ // 001042663 NM_ // 042664 NM_ // 001042665 NM_ // NM_ 198681 NM_ // 001008564 NM_ // 001008565 NM_

45 WSB1 NFKBIE NM_ TNFRSF25 // TNFRSF25 PLEKHG5

50 containing 8 containing TRIMB NM_

55 tripartite motif- tripartite box- SOCS and repeat WD 1 containing nucleoporin like 1 like nucleoporin light of kappa factor nuclear in B- enhancer gene polypeptide epsilon inhibitor, cells NUPL1 tumor necrosis factor receptor receptor factor necrosis tumor // 25 member superfamily, domain homology pleckstrin (with G family containing, RhoGef domain) member 5 Gene Name Gene Symbol Accession Synonym

304 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3608113 chr15 + 88732454 88846463 1.04 2492064 chr2 + 86509150 86574548 1.04 2358171 chr1 + 148560583 148592321 1.04 Transcript Transcript ID Cluster 3853453 chr19 - 15423181 15436377 1.04 3337618 chur11 + 67984785 68173381 1.04 Human ST Exon 1.0

30 (continued) HUMORFA01 // HUMORFA01 // SAR1 KlAA0051 p195 DKFZp686A24246 DKFZp686A24246 // DKFZp686P07111 // JHMD2A // JMJD1 // HPRP3 // HPRP3P HPRP3P // HPRP3 // // Prp3p PRP3 // // // FLJ32145 RP18 HSPC099 DKFZp667E013 // DKFZp667E013 FLJ00087 - 2878437 chr5 - 139991507 139993422 1.04 35 // C11orf23 DKFZp781E17107 DKFZp781E2314 // DKFZp78102362 // // FLJ11058 // // FLJ43065 // MGC125711 // MGG125712 // SAP190 // PP6R3 SAPLa // SAPL 003870 012448 STAT5 018433 3757770 chr17 - 37604727 37682109 1.04 004698 000591 018312 029084 NM_ // NM_ 015203 40 NM_ // NM_ 001040021

45 IQGAP1 NM_ STAT5B NM_ PRPF3 // KIAA0460

50 mRNA processing 55 1Q motif containing GTPase GTPase containing motif 1Q 1 protein activating jumonji domain containing 1A containing domain jumonji JMJD1A NM_ signal transducer and activator activator and transducer signal transcription of CD14 moleculeCD14 PRP3 pre- factor 3 homolog(S.cerevisiae) // KIAA0460 CD14 hypothetical protein FLJ21438protein hypothetical FLJ21438 XM_ SAPS domain family, member 3 member family, domain SAPS SAPS3 NM_ Gene Name Gene Symbol Accession Synonym

305 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3633403 chr15 - 73448786 73535167 1.04 2346934 chr1 + 93147511 93377202 1.04 3046197 chr7 - 36860492 37455389 1.04 3956290 chr22 - 26577440 26645487 1.04 2621275 chr3 + 47298888 47367590 1.04 2709062 chr3 - 187048509 187160523 1.04 2829275 chr5 + 133734769 133788148 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) beta // // beta 1 // 1 beta // beta 12 // 12 CED12 // TP- DKFZP434K2235 // DKFZP434K2235 // FLJ90319 KIAA0700 M96 // PCL2 // // RP5-976013.1 dJ976013.2 CED- ELMO- // MGC KlAA0281 126406 PI- // VIB1B PtdlnsTP FLJ13703 // FLJ13703 KWA0795 DKFZp686F18120 DKFZp686F18120 // Htra2- // TRA2- SRFS10 TRA2B // BETA 35 HHR6B E2-17kDa // // HR6B // RAD6B // UBC2 015477 002110 JTK9 3881651 chr20 + 30086433 30153306 1.04 007358 006662 KIAA0309 3656418 chr16 + 30616551 30663998 1.04 014800 012399 013345 // MGC99642 G2A 3581404 chr14 - 104586779 104622593 1.04 025010 004593 003337

40 NM_ // 001039459 NM_ // NM_ 130442

45 SIN3A NM_ MTF2 NM_ SRCAP NM_ PITPNB NM_ SFRS10 NM_ UBE2B NM_

50 serine- coupled receptor 132 GPR132 NM_ 55 enzyme conjugating like 18 (Drosophila) KLHL18 NM_ related CBP activator CBP activator related (A) polymerase alpha (A) polymerase PAPOLA 032632 NM PAP // MGC5378 3550392 chr14 + 96038038 96104627 1.04 SIN3 homolog A, transcription A, transcription homolog SIN3 (yeast) regulator hemopoietic cell kinase cell hemopoietic HCK NM_ engulfment and cell motility 1 motility cell and engulfment ELMO1 metal response element binding binding element response metal 2 factor transcription Snf2- protein phosphatidylinositol transfer transfer phosphatidylinositol beta protein, G protein- G poly kelch- rich 10 (transformer 2 homolog, 2 homolog, 10 (transformer rich Drosophila) splicing factor, arginine/ factor, splicing ubiquitin- (RAD6 homolog) E2B Gene Name Gene Symbol Accession Synonym

306 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3791168 chr18 + 58005478 58125326 1.04 3003193 chr7 + 56086894 56099148 1.04 3301857 chr10 - 98267858 98337079 1.04 2987441 chr7 + 2315929 2386896 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0 1- 30 P116 // P116 (continued) iso // 2 // TCP- // 2 P- 5 2422035 chr1 - 89496930 89511122 1.04 ETA // EIF3- // EIF3- ETA zeta // CCT- // zeta 1 // APA1 1 // 3543884 chr14 + 73423093 73468718 1.04 1 // CCT6 // CCT6 1 // FLJ33841 // FLJ33841 // HsT885 HsT3308 zeta // TCP20 // TCP20 // zeta TTCP20 // TCPZ CCT- zeta- // // HTR3 Cctz // MGC126214 // MGC126215 MoDP- EP70- // RP11-34E5.1 SMBP 35 EIF3- EIF3- // P110 // MGC104664 // MGC131875 eIF3b // PRT1 021188 APA- 020854 015934 HSPC120 2523144 chr2 + 202811346 202926967 1.04 001762 024097 MGC955 2332767 chr1 + 43005527 43036633 1.04 020123 003751 NM_ // 001009186 NM_ 40 NM_ // 001037283 NM_

45 CCT6A C1orf50 NM_ TM9SF3 NM_ EIF3S9

55 3’ exoribonuclease 2 exoribonuclease 3’ XRN2 012255 NM - 3879467 chr20 + 21219705 21322172 1.04 ’- KIAA1468 NOP5/NOP58 protein nucleolar NOP5/NOP58 NM_ 5 KIAA1468 NM_ guanylate binding protein 5 protein binding guanylate GBP5 052942 NM GBP- zinc finger protein 410 protein finger zinc ZNF410 NM_ chaperonin containing TCP1, TCP1, containing chaperonin 1) 6A (zeta subunit chromosome 1 open reading reading open 1 chromosome frame 50 transmembrane 9 superfamily member 3 eukaryotic translationinitiation 116kDa eta, 9 subunit 3, factor Gene Name Gene Symbol Accession Synonym

307 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 7 - 141273626 141298905 1.04 Chrom osome Human Genome hg18 Genome Human

25 3647956 ehr16 + 10729448 10771777 1.04 3076868 chr. 3504434 chr13 -2622359 chr3 20251014 20375187 + 1.04 49942372 50089683 1.04 2999948 chr7 + 44612716 44715181 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0

30 12 // 12 3 // 3 // (continued) LU- 1 // DBC1 1 3089597 chr8 + 22518038 22534618 1.04 MGC117406 // MGC117406 // MGC130052 NBP // MGC130053 NBP1 // CLECSF5 // MDL- // MDL- 1 CLECSF5 // MDL1 // MGC138304 // FLJ13046 KIAA1721 DEF- // 3G2 // DEF3 // DKFZp686B0877 // HLC- FLJ36517 11 // NY- g16 AKGDH // E1k // E1k // AKGDH OGDC DBC- 35 - 2654394 chr3 + 182113040 182179459 1.04 002484 013252 022459 005777 002541 021174 005087 NM- // 001003941 NM_ NM_ // NM_ 199205 40 NM // 001013438 NM_ // 001013439 NM_

45 NUBP1 NM_ CLEC5A NM_ OGDH FXR1

55 type lectin domain family 5, 5, family domain lectin type RNA binding motif protein 6 RBM6 1 protein binding nucleotide E. coli) homolog, (MinD NM_ exportin 4exportin XPO4 NM_ KIAA1967 KIAA1967 C- member A ketoglutarate) dehydrogenase dehydrogenase ketoglutarate) (lipoamide) oxoglutarate (alpha- oxoglutarate fragile X mental retardation, retardation, mental X fragile 1 homolog autosomal Gene Name Gene Symbol Accession Synonym

308 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3820443 chr19 +3220513 chr9 10242765 10258289 - 1.04 113131941 113286475 1.04 2929036 chr6 + 144194149 144227146 1.04 2954646 chr6 - 43587500 43592701 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) DELTA // T3D DELTA 3393744 chr11 - 117698596 117718659 1.04 CD3- BB2 // CD54 // CD54 // // BB2 P3.58 FLJ22036 // ECM29 // K1AA1962 // RP11- dJ468K18.5 // dJ468K18.5 // C6orf93 // FLJ14909 dJ468K18.4 35 // C6orf109 // DKFZP566C243 // KUP1 FinGER3 // dJ337H4.3 // // FLJ44836 // MGC131686 dJ337H4.2 014820 FLJ90470 2686371 chr3 - 101565001 101614635 1.04 000732 000201 032860 015388 928657 928657 NM_ // NM 001040651 XM_ // 001129450 XM_ // 001131778 NM_ 001080398 XM_ // XM_ // 941265 NM_ 40 NM_ // NM_ 001012974

45 TOMM70A NM_ CD3D ICAM 1 NM_ C6orf94 // LTV1 C6orf94 YIPF3 // YIPF3 C6orf154

55 translocase of outer outer of translocase mitochondrial membrane 70 A cerevisiae) (S. KIAA0368delta (CD3- molecule, CD3d KIAA0368 TCR complex) intercellular adhesion molecule molecule adhesion intercellular rhinovirus human (CD54), 1 receptor chromosome 6 open reading reading open 6 chromosome frame 94 // LTV1 homolog (S. cerevisiae) Yip1 domain family, member 3 3 member family, domain Yip1 reading open 6 chromosome // frame 154 Gene Name Gene Symbol Accession Synonym

309 EP 2 136 209 A1

5 Fold Change /nM

15 Strand Start Stop

20 Chrom osome Human Genome hg18 Genome Human

25 3833291 chr19 + 45168772 45179181 1.04 2394784 chr1 - 6504004 6537329 1.04 2619344 chr3 + 42617105 42678166 1.04 Transcript Transcript ID Cluster Human ST Exon 1.0

30 (continued) MGC13687 // MGC13687 // MGC23214 // MGC8570 // // S6 MIP224 FLJ23323 // FLJ23323 // MGC131821 MGC138483 35 // DKFZp686F1754 // DKFZp686G0426 DKFZp686J06106 // DKFZp686N24126 006503 024654 005385 NM_ // NM_ 153001 40 NM_ // 001012651 NM_

45 PSMC4 NKTR

50 tumor

55 proteasome (prosome, (prosome, proteasome subunit, 26S macropain) 4 ATPase, nucleolar protein 9 protein nucleolar NOL9 NM_ homolog natural killer- natural homolog recognition sequence Gene Name Gene Symbol Accession Synonym

310 EP 2 136 209 A1

311 EP 2 136 209 A1

312 EP 2 136 209 A1

313 EP 2 136 209 A1

314 EP 2 136 209 A1

315 EP 2 136 209 A1

316 EP 2 136 209 A1

317 EP 2 136 209 A1

318 EP 2 136 209 A1

319 EP 2 136 209 A1

320 EP 2 136 209 A1

321 EP 2 136 209 A1

322 EP 2 136 209 A1

323 EP 2 136 209 A1

35 Claims

1. A method for assaying an action of a compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a solvate of them to a mammal, which comprises detecting splicing defect caused by the compound represented by formula (I), the pharmaceutically acceptable salt thereof, or the solvate of them: 40

55 wherein R3, R6, R7 and R21, the same or different, each represents

1) a hydroxyl group or an oxo group formed together with the carbon atom to which it is bound, provided that

324 EP 2 136 209 A1

R6 is limited to a hydroxyl group,

2) an optionally substituted C1-22 alkoxy group, 3) an optionally substituted unsaturated C2-22 alkoxy group, 4) an optionally substituted C7-22 aralkyloxy group, 5 5) an optionally substituted 5- to 14-membered heteroaralkyloxy group, 6) RCO-O- wherein R represents

a) a hydrogen atom, b) an optionally substituted C1-22 alkyl group, 10 c) an optionally substituted unsaturated C2-22 alkyl group, d) an optionally substituted C6-14 aryl group, e) an optionally substituted 5- to 14-membered heteroaryl group, f) an optionally substituted C7-22 aralkyl group, g) an optionally substituted 5- to 14-membered heteroaralkyl group, 15 h) an optionally substituted C1-22 alkoxy group, i) an optionally substituted unsaturated C2-22 alkoxy group, j) an optionally substituted C6-14 aryloxy group or k) an optionally substituted 5- to 14-membered heteroaryloxy group,

20 7) RS1 RS2RS3SiO- wherein RS1, RS2, and RS3, the same or different, each represents

a) a C1-6 alkyl group or b) a C6-14 aryl group,

25 8) a halogen atom, 9) RN1RN2N-RM- wherein RM represents

a) a single bond, b) -CO-O-, 30 c) -SO2-O-, d) -CS-O-or N3 N3 e) -CO-NR - wherein R represents a hydrogen atom or an optionally substituted C1-6 alkyl group, provided that each of the leftmost bond in b) to e)is bound to the nitrogen atom; and RN1 and RN2, the same or different from each other and each represents 35 a) a hydrogen atom, b) an optionally substituted C1-22 alkyl group, c) an optionally substituted unsaturated C2-22 alkyl group, d) an optionally substituted aliphatic C2-22 acyl group, 40 e) an optionally substituted aromatic C7-15 acyl group, f) an optionally substituted C6-14 aryl group, g) an optionally substituted 5- to 14-membered heteroaryl group, h) an optionally substituted C7-22 aralkyl group, i) an optionally substituted C1-22 alkylsulfonyl group, 45 j) an optionally substituted C6-14 arylsulfonyl group, k) an optionally substituted 3- to 14-membered non-aromatic heterocyclic group formed by RN1 and RN2 together with the nitrogen atom to which RN1 and RN2 are bound, and the non-aromatic heterocyclic group optionally has substituent(s), l) an optionally substituted 5- to 14-membered heteroaralkyl group, 50 m) an optionally substituted C3-14 cycloalkyl group or n) an optionally substituted 3- to 14-membered non-aromatic heterocyclic group,

N4 N4 10) R SO2-O-wherein R represents

55 a) an optionally substituted C1-22 alkyl group, b) an optionally substituted C6-14 aryl group, c) an optionally substituted C1-22 alkoxy group, d) an optionally substituted unsaturated C2-22 alkoxy group,

325 EP 2 136 209 A1

e) an optionally substituted C6-14 aryloxy group, f) an optionally substituted 5- to 14-membered heteroaryloxy group, g) an optionally substituted C7-22 aralkyloxy group or h) an optionally substituted 5- to 14-membered heteroaralkyloxy group, 5 N5 N5 11) (R O)2PO-O- wherein R represents

a) an optionally substituted C1-22 alkyl group, b) an optionally substituted unsaturated C2-22 alkyl group, 10 c) an optionally substituted C6-14 aryl group, d) an optionally substituted 5- to 14-membered heteroaryl group, e) an optionally substituted C7-22 aralkyl group or f) an optionally substituted 5- to 14-membered heteroaralkyl group,

15 N1 N2 N1 N2 12) (R R N2PO-O- wherein R and R have the same meanings as defined above or 13) (RN1RN2N)(RN5O)PO-O- wherein RN1, RN2 and RN5 have the same meanings as defined above, provided that a compound in which R3, R6, R7 and R21 are all hydroxyl groups, and a compound in which R3, R6 and R21 are all hydroxyl groups and R7 is an acetoxy group are excluded, R16 represents a hydrogen atom or hydroxyl group. 20 2. The method according to claim 1, wherein the compound represented by formula (I) is selected from the group consisting of:

(8E,12E,14E)-7-(N-(2-(N’,N’-Dimethylamino)ethyl)-N-methylcar bamoyloxy)-3,6,16, 21-tetra hydroxy-6,10,12, 25 16, 20-pentamethyl -18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahyd roxy-6,10,12,16,20-pentameth yl-7-((4-methylhomopiperazin-1-yl)carbonyl) oxy-18,19-epoxytri cosa-8,12,14-trien-11-olide; (8E,12E,14 E)-3,6,16, 21-Tetrahydroxy-6,10,12,16,20-pentameth yl-7-((4-methylpiperazin-1-yl)carbonyl)oxy- 18,19-epoxytricosa-8,12,14-trien-11-olid e; 30 (8E,12E,14E)-7-((4-Butylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16, 20-pentamethyl-18, 19-epoxytricosa-8, 12,14-trien-11-olide; (8E,12E,14E)-7-((4-Ethylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl- 18,19-epoxytricosa-8, 12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-6,10,12,16,20-pentameth yl-7-((4-propylpiperazin-1-yl)carbonyl)oxy- 35 18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Cyclohexylpiperazin-1-yl)carbonyl)oxy-3,6,1 6,21-tetrahydroxy-6,10,12,16,20-pentame-- thyl-18,19-epoxytrico sa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-(Cyclopropylmethyl)piperazin-1-yl)carbonyl) oxy-3, 6,16, 21-tetrahydroxy-6,10,12,16, 20-pentamethyl-18,19-epoxytricosa -8,12,14-trien-11-olide; 40 (8E,12E,14E)-3,6,16,21-Tetrahydroxy-6,10,12,16,20-pentameth yl-7-((4-propylhomopiperazin-1-yl)carbonyl) oxy-18,19-epoxytric osa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-(Cyclopropylmethyl)homopiperazin-1-yl)car bonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytric osa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Cyclopentylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-tetrahydroxy-6,10,12,16,20-pentame- 45 thyl-18,19-epoxytric osa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-7-((4-isopropylpiperazin-1-yl)carbonyl)oxy-6,10,12,16,20-pentamethyl- 18,19-epoxytrico sa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6, 16,21-Tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytric osa-8,12,14-trien-11-olide; 50 (8E,12E,14E)-7-(N-(2-(N’,N’-Diethylamino)ethyl)-N-methylcarba moyloxy)-3,6,16,21-tetrahydroxy-6,10,12,16, 20-pentamethyl-1 8,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-7-((4-isobutylhomopipera zin-1-yl)carbonyl)oxy-6,10,1 2,16,20- pentamethyl-18,19-epoxyt ricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Ethylhomopiperazin-1-yl)carbonyl)oxy-3,6,1 6,21-tetrahydroxy-6,10,12,16,20-pentame- 55 thyl-18,19-epoxytrico sa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Butylhomopiperazin-1-yl)carbonyl)oxy-3,6,1 6,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytrico sa-8,12,14-trien-11-olide; (8E,12E,14E)-3,16, 21-Trihydroxy-6-methoxy-6,10,12,16,20-pen tamethyl-7-((4-methylpiperazin-1-yl)carbon-

326 EP 2 136 209 A1

yl)oxy-18,19-epoxyt ricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,16, 21-Trihydroxy-6-methoxy-6,10,12,16,20-pen tamethyl-7-((4-(piperidin-1-yl)piperidin-1-yl) carbonyl)oxy-18,1 9-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14 E)-3,6, 7, 21-Tetrahydroxy-6,10,12,16, 20-pentamethyl -18,19-epoxytricosa-8,12,14-trien-11-olide; 5 (8E,12E,14E)-7-((4-(2,2-Dimethylpropyl)homopiperazin-1-yl)car bonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12, 16,20-pentamethyl-1 8,19-epoxytricosa-8,12,14-trien-11-olide; and (8E,12E,14E)-3, 6,16-Trihydroxy-21-methoxy-6,10,12,16,20-pen tamethyl-7-((4-methylpiperazin-1-yl) carbonyl) oxy-18,19-epoxyt ricosa-8,12,14-trien-11-olide.

10 3. The method according to claim 1, wherein the detection of splicing defect comprises the steps of:

(a) measuring the expression level of pre-mRNA before and after administration of the compound represented by formula (I), the pharmaceutically acceptable salt thereof ,or the solvate of them to a mammal; (b) comparing, based on the expression level measured in (a), the expression level of pre-mRNA before and 15 after administration of the compound represented by formula (I), the pharmaceutically acceptable salt thereof, or the solvate of them, to determine that the compound represented by formula (I), the pharmaceutically acceptable salt thereof, or the solvate of them exerts an action to the mammal when the expression level of pre- mRNA after the administration increases.

20 4. The method according to claim 3, wherein the pre-mRNA of which expression level is measured is pre-mRNA of at least one gene selected from the genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5, or a homologous gene thereof.

5. The method according to claim 4, wherein the gene(s) are selected from DNAJB1, BZW1, NUP54, RIOK3, CDKN1B, 25 STK17B, EIF4A1, and ID1.

6. The method according to claim 3, wherein in step (a), the expression level of pre-mRNA in samples obtained from a subject before and after administration of the compound represented by formula (I), the pharmaceutically acceptable salt thereof, or the solvate of them, is measured. 30 7. The method according to claim 6, wherein the samples obtained from the subject are selected from hemocytes in peripheral blood, plasma, and serum.

8. A probe or primer for assaying an action of a compound represented by formula (I), a pharmaceutically acceptable 35 salt thereof, or a solvate of them to a mammal, which consists of a polynucleotide capable of hybridizing with a polynucleotide consisting of a nucleotide sequence of at least one gene selected from the genes listed in Table 1, Table 2, Table 3, Table 4, and Table 5, and a homologous gene thereof, or a complementary sequence thereof.

9. The probe or primer according to claim 8, which is capable of detecting a genomic intron region or a part thereof in 40 a gene listed in Table 1, Table 2, Table 3, Table 4 and Table 5, or which is capable of detecting a polynucleotide lacking a part of a genomic exon region in a gene listed in Table 1, Table 2, Table 3, Table 4 and Table 5.

10. A reagent or kit for assaying an action of a compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a solvate of them to a mammal, which comprises the probe or the primer according to claim 8. 45 11. The method according to claim 1, wherein the detection of splicing defect comprises the steps of:

(f) measuring the expression level of an abnormal protein before and after administration of the compound represented by formula (I), the pharmaceutically acceptable salt thereof, or the solvate of them to a mammal; 50 (g) comparing, based on the expression level measured in (f), the expression level of the abnormal protein before and after administration of the compound represented by formula (I), the pharmaceutically acceptable salt thereof or the solvate of them, to determine that the compound represented by formula (I), the pharmaceutically acceptable salt thereof, or the solvate of them exerts an action to the mammal when the expression level of the abnormal protein after the administration increases. 55 12. The method according to claim 11, wherein the abnormal protein of which expression level is measured is a protein consisting of amino acids encoded by a polynucleotide of at least one gene selected from the genes listed in Table 1 and Table 3, or a homologous gene thereof where splicing defect has been caused in the polynucleotide, or a

327 EP 2 136 209 A1

protein consisting of amino acids encoded by a polynucleotide of at least one gene selected from the genes listed in Table 2, Table 4 and Table 5 or a homologous gene thereof where splicing defect has been caused in the polynucleotide.

5 13. The method according to claim 11, wherein the abnormal protein of which expression level is measured is a protein consisting of amino acids encoded by a polynucleotide of at least one gene selected from DNAJB1, BZW1, NUP54, RIOK3, CDKN1B, STK17B, EIF4AI and ID1 where splicing defect has been caused in the polynucleotide.

14. The method according to claim 11, wherein in step (f), the expression level of the abnormal protein in the samples 10 obtained from a subject before and after administration of the compound represented by formula (I) or the pharmaceutically acceptable salt thereof or the solvate of them, is measured.

15. The method according to claim 14, wherein the samples obtained from the subject are selected from hemocytes in peripheral blood, plasma, and serum. 15 16. An antibody against an abnormal protein consisting of amino acids encoded by a polynucleotide of at least one gene selected from the genes listed in Table 1, Table 2, Table 3, Table 4 and Table 5 where splicing defect has been caused in the polynucleotide, or a fragment thereof.

20 17. A reagent or kit for assaying an action of a compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a solvate of them to a mammal, comprising the antibody or the fragment thereof according to claim 16.

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REFERENCES CITED IN THE DESCRIPTION

This list of references cited by the applicant is for the reader’s convenience only. It does not form part of the European patent document. Even though great care has been taken in compiling the references, errors or omissions cannot be excluded and the EPO disclaims all liability in this regard.

Patent documents cited in the description

• WO 2002060890 A [0002] • WO 0028082 A [0072] • WO 2003099813 A [0002] • JP 60500684 T [0092]

Non-patent literature cited in the description

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