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Q2 2020 XPEDITE Portfolio Our XPEDITE List Primarily Consists of More Demanding Targets, for Which We Have Established In- House Protocols for Crystallization

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Q2 2020 XPEDITE Portfolio Our XPEDITE list primarily consists of more demanding targets, for which we have established in- house protocols for crystallization. In addition, this service grants you quick access to ligand-target protein complex structures, when the crystallization conditions are well described in the literature. XPEDITE service also include the work on disease relevant mutations of established targets and the optimization of published but low resolution structures. Established and/or published conditions Few hundred disease-relevant targets Average 4 months turn-around Protein Name UniProt Identifier Protein Name UniProt Identifier ABCB10 Q9NRK6 AURKA O14965 ACACB O00763 AURKB Q96GD4 ACLY P53396 Barstar P11540 ACVR1B P36896 BAX Q07812 ADORA2A P29274 BAZ1A Q9NRL2 AK1 p00568 BCAT1 P54687 AKT2 P31751 BCL2 P10415 AKT3 Q9Y243 BCL2L1 Q07817 ALK Q9UM73 β-Lactoglobulin P02754 ALPK1 Q96QP1 BirA P06709 ASGR2 P07307 BIRC2 Q13490 ATAD2 Q6PL18 BRDT Q58F21 ATAD2B Q9ULI0 Bromelain P14518 ATM Q13315 BTK Q06187 ATR Q13535 BUB1 O43683 ATRIP Q8WXE1 CAMKK2 Q96RR4 1 Q2 2020 Protein Name UniProt Identifier Protein Name UniProt Identifier CANX P27824 CKS2 P33552 Caspase3 P42574 CNR1 P21554 CCM2 Q9BSQ5 Comt P22734 CCM3 Q9BUL8 CRISP-3 O19010 CCNA2 P20248 Csk P32577 CCNC P24863 CTNB1 P35222 CCNH P51946 CTSB P07858 CCNK O75909 CTSC P97821 CD3D P04234 CTSK O35186 CD3E P07766 CTSL1 P07711 CD3G P09693 CUL4A Q13619 CDC37 Q16543 cybC P0ABE7 CDK8 P49336 DBF4 Q9UBU7 CDK8/CycC unknown DDB1 Q16531 CDKL1 Q00532 DDR1 Q08345 CDKL2 Q92772 DDX58 O95786 CDKL5 O76039 dgoT P0AA76 CDT1 Q9H211 DHODH Q02127 CETP P11597 DNAJB1 P25685 CFTR A0M8U4 DNM1L O00429 CHD4 Q14839 DOCK5 Q9H7D0 CHK1 O14757 DOT1L Q8TEK3 CK1_3 Q9Y6M4 DYRK1B Q9Y463 CKS1B P61024 DYRK2 Q92630 2 Q2 2020 Protein Name UniProt Identifier Protein Name UniProt Identifier DYRK3 O43781-2 FFAR1 O14842 DYRK4 Q9NR20 FGFR2 P21802 E4PDH P0A9B6 FKBP12 P62942 EED O75530 FKBP5 Q13451 EGLN1 Q9GZT9 Flt-1 P17948 EGLN2 Q96KS0 FNTA P49354 EGLN3 Q9H6Z9 FNTB P49356 EHMT2 Q96KQ7 FURIN P09958 EIF2A Q9BY44 GAK O14976 EIF2AK3 Q9NZJ5 GCGR P47871 EIF2S1 P05198 GFP P42212 ELB P16278-2 GIPR P48546 EME1 Q96AY2 GLB1 P16278 EphA3 P29320 GLI1 P08151 EphA7 Q15375 GNAS P63092 EPHB1 P54762 GP6 A0A2K5VXN2 EphB4 P54760 Grap2 O89100 EXO1 Q9UQ84 GRM1 Q13255 EZH2 Q15910 GRM5 P41594 F3 P13726 GRM7 Q14831 F8 P00451 GSK3A P49840 FBXO17 Q96EF6 HAT1 O14929 FER P16591-2 HCK P08631 FES P07332 HDAC-1 Q13547 3 Q2 2020 Protein Name UniProt Identifier Protein Name UniProt Identifier HDAC-10 Q969S8 JMJD1A Q9Y4C1 HDAC-6 Q9UBN7 JMJD2E B2RXH2 HPGD P15428 JMJD6 Q6NYC1 HRAS P01112 KDM8 Q8N371 HRV-B H9EHM4 KHDRBS1 Q07666 HRV-C G8IJF5 KHDRBS2 Q5VWX1 HS2ST1 Q7LGA3 KSR1 Q8IVT5 HSPA5_m P20029 KSR2 Q6VAB6 HUS1 O60921 L3MBTL1 Q9Y468 IDH2 P48735 L3MBTL2 Q969R5 IFIH1 Q9BYX4 L3MBTL3 Q96JM7 IKK2 O14920 Lamtor2 Q9JHS3 IL17A Q16552 LDHA P00338 IL18R1 Q13478 LIG1 P18858 IL18RAP O95256 LIG3 P49916 IL1RL1 Q01638 LIMK1 P53667 IL2 P60568 Lipolase unknown IL2RA P01589 LLC P03772 IL2RB P14784 LPXC_ECOLI P0A725 IL2RG P31785 LPXC_NEIG1 Q5F569 IL7R P16871 LPXC_PSEAE P47205 IRF4 Q15306 LRRK2 Q5S007 ITGAV P06756 MAOB P19643 ITGB1 P05556 Map2K4 P45985 4 Q2 2020 Protein Name UniProt Identifier Protein Name UniProt Identifier MAP2K5 Q13163 NR4A1 P22736 Map2K7 O14733 NR5A2 O00482 MAP3K14 Q99558 NRDP1 Q9H4P4 MAP3K5 Q99683 NTRK3 Q16288 MAP4K4 O95819 NTSR1 P30989 MapK13 Q9Z1B7 P2RX3 P56373 MAX P61244 PADI2 Q9Y2J8 MBD3 O95983 PAK1 Q13153 MDM2 Q00987 PAK6 Q9NQU5 MELK Q14680 PAK7 Q9P286 MKNK1 Q9BUB5 Parp-12 Q9H0J9 MLST8 Q9BVC4 Parp-14 Q460N5 MTA1 Q13330 Parp-15 Q460N3 MUS81 Q96NY9 Parp-3 Q9Y6F1 MYD88 Q99836 PAS Q96RG2 MYST1 Q9H7Z6 PBRM1 Q86U86 NEDD4 P46934 PC P11498 NEK7 Q8TDX7 PDE3B Q13370 NFKB1 P19838 PDE6D O43924 NLRP3 Q96P20 PDK1 Q15118 NMT1 P30419 PDK2 Q15119 NO66 Q9H6W3 PDK3 Q15120 NOD2 Q9HC29 PDK4 Q16654 NR2F6 P10588 PDPK1 O15530 5 Q2 2020 Protein Name UniProt Identifier Protein Name UniProt Identifier PF3D7_0515300 Q8I3V5 PRKAG2 Q9UGJ0 PF4 A0A2K5V1A0 PRKAG3 Q9UGI9 PGGT1B P53609 PRMT3 O60678 PHKG2 P15735 PRMT5 O14744 PIK3CD O00329 PTK2B Q14289 PIK3R1 P27986 PTK6 Q13882 PKCtheta Q04759 PYGL P06737 PKM2 P14618 QPCTL Q9NXS2 PKMYT1A Q99640 RAC1 P63000 PLA2G16 P53816 RAD1 O60671 Plk-1 Q4KMI8 RAD9A Q99638 Plk-4 O00444 RAF1 P04049 POLQ O75417 RARA P10276 PPARA Q07869 RBBP4 Q09028 PPARD Q03181 RBBP7 Q16576 PPARG P37231 RBX1 P62877 PPID Q08752 RCOR1 Q9UKL0 PPP1CA P62136 REL Q04864 PPP2R1A P30153 RIPK1 Q13546 PPP5C P53041 RIPK2 O43353 PRDM10 Q9NQV6 Ron Q04912 PRKAB1 Q9Y478 RORA P35398 PRKAB2 O43741 RORB Q92753 PRKAG1 P54619 RSK2 P51812 6 Q2 2020 Protein Name UniProt Identifier Protein Name UniProt Identifier RTF1 Q92541 STAT3 P40763 Rub P24297 STK33 Q9BYT3 RXRA P19793 STK4 Q13043 SARM1 Q6SZW1 STY8 O22558 SB11 Q46731 Subtilisin P00780 SGK1 O00141 SUI2 P20459 SH2D1A O60880 TAF1L Q8IZX4 SIK2 Q9H0K1 TASP1 Q9H6P5 SIRT1 Q96EB6 TBK1 Q9UHD2 SIRT5 Q9NXA8 TCEB1 Q15369 SIRT7 Q9NRC8 TCEB2 Q15370 SKP1 P63208 TET1 Q8NFU7 SLC2A1 P11166 TET2 Q6N021 SMARCA1 P28370 TET3 O43151-4 SMARCA5 O60264 THRA P10827 SMARCA6 Q9NRZ9 THRB P10828 SMARCC1 Q92922 TKTL1 Q99MX0 SMARCC2 Q8TAQ2 TKTL2 Q9H0I9 SMYD2 Q9NRG4 TLR3 O15455 SMYD3 Q9H7B4 TLR7 Q9NYK1 SND Q5FPV1 TLX Q9Y466 SNRPC P09234 Tmem173 Q3TBT3-3 SOS1 Q07889 TNF P01375 SPSB4 Q96A44 TNFRSF9 Q07011 7 Q2 2020 Protein Name UniProt Identifier Protein Name UniProt Identifier TNKS2 Q9H2K2 USP2 O75604 TOPBP1 Q92547 USP8 P40818 TP53 P04637 VEGF-R2 P35968 TREM2 Q9NZC2 VHL P40337 TUBA1B P81947 VP0 Q82122 TUBB2B Q6B856 WDR48 Q8TAF3 TYR P14679 WDR77 Q9BQA1 UBB P0CG47 WHSC1L1 Q9BZ95 ULK1 O75385 WRN Q14191 ULK2 Q8IYT8 XRN1 Q8IZH2 ULK3 Q6PHR2 ZC3H12A Q5D1E8 USP19 O94966 8 .
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  • Profiling Data

    Profiling Data

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  • Lipid Metabolic Reprogramming: Role in Melanoma Progression and Therapeutic Perspectives

    Lipid Metabolic Reprogramming: Role in Melanoma Progression and Therapeutic Perspectives

    cancers Review Lipid metabolic Reprogramming: Role in Melanoma Progression and Therapeutic Perspectives 1, 1, 1 2 1 Laurence Pellerin y, Lorry Carrié y , Carine Dufau , Laurence Nieto , Bruno Ségui , 1,3 1, , 1, , Thierry Levade , Joëlle Riond * z and Nathalie Andrieu-Abadie * z 1 Centre de Recherches en Cancérologie de Toulouse, Equipe Labellisée Fondation ARC, Université Fédérale de Toulouse Midi-Pyrénées, Université Toulouse III Paul-Sabatier, Inserm 1037, 2 avenue Hubert Curien, tgrCS 53717, 31037 Toulouse CEDEX 1, France; [email protected] (L.P.); [email protected] (L.C.); [email protected] (C.D.); [email protected] (B.S.); [email protected] (T.L.) 2 Institut de Pharmacologie et de Biologie Structurale, CNRS, Université Toulouse III Paul-Sabatier, UMR 5089, 205 Route de Narbonne, 31400 Toulouse, France; [email protected] 3 Laboratoire de Biochimie Métabolique, CHU Toulouse, 31059 Toulouse, France * Correspondence: [email protected] (J.R.); [email protected] (N.A.-A.); Tel.: +33-582-7416-20 (J.R.) These authors contributed equally to this work. y These authors jointly supervised this work. z Received: 15 September 2020; Accepted: 23 October 2020; Published: 27 October 2020 Simple Summary: Melanoma is a devastating skin cancer characterized by an impressive metabolic plasticity. Melanoma cells are able to adapt to the tumor microenvironment by using a variety of fuels that contribute to tumor growth and progression. In this review, the authors summarize the contribution of the lipid metabolic network in melanoma plasticity and aggressiveness, with a particular attention to specific lipid classes such as glycerophospholipids, sphingolipids, sterols and eicosanoids.
  • (12) Patent Application Publication (10) Pub. No.: US 2003/0082511 A1 Brown Et Al

    (12) Patent Application Publication (10) Pub. No.: US 2003/0082511 A1 Brown Et Al

    US 20030082511A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2003/0082511 A1 Brown et al. (43) Pub. Date: May 1, 2003 (54) IDENTIFICATION OF MODULATORY Publication Classification MOLECULES USING INDUCIBLE PROMOTERS (51) Int. Cl." ............................... C12O 1/00; C12O 1/68 (52) U.S. Cl. ..................................................... 435/4; 435/6 (76) Inventors: Steven J. Brown, San Diego, CA (US); Damien J. Dunnington, San Diego, CA (US); Imran Clark, San Diego, CA (57) ABSTRACT (US) Correspondence Address: Methods for identifying an ion channel modulator, a target David B. Waller & Associates membrane receptor modulator molecule, and other modula 5677 Oberlin Drive tory molecules are disclosed, as well as cells and vectors for Suit 214 use in those methods. A polynucleotide encoding target is San Diego, CA 92121 (US) provided in a cell under control of an inducible promoter, and candidate modulatory molecules are contacted with the (21) Appl. No.: 09/965,201 cell after induction of the promoter to ascertain whether a change in a measurable physiological parameter occurs as a (22) Filed: Sep. 25, 2001 result of the candidate modulatory molecule. Patent Application Publication May 1, 2003 Sheet 1 of 8 US 2003/0082511 A1 KCNC1 cDNA F.G. 1 Patent Application Publication May 1, 2003 Sheet 2 of 8 US 2003/0082511 A1 49 - -9 G C EH H EH N t R M h so as se W M M MP N FIG.2 Patent Application Publication May 1, 2003 Sheet 3 of 8 US 2003/0082511 A1 FG. 3 Patent Application Publication May 1, 2003 Sheet 4 of 8 US 2003/0082511 A1 KCNC1 ITREXCHO KC 150 mM KC 2000000 so 100 mM induced Uninduced Steady state O 100 200 300 400 500 600 700 Time (seconds) FIG.
  • Inhibition of Mitochondrial Complex II in Neuronal Cells Triggers Unique

    Inhibition of Mitochondrial Complex II in Neuronal Cells Triggers Unique

    www.nature.com/scientificreports OPEN Inhibition of mitochondrial complex II in neuronal cells triggers unique pathways culminating in autophagy with implications for neurodegeneration Sathyanarayanan Ranganayaki1, Neema Jamshidi2, Mohamad Aiyaz3, Santhosh‑Kumar Rashmi4, Narayanappa Gayathri4, Pulleri Kandi Harsha5, Balasundaram Padmanabhan6 & Muchukunte Mukunda Srinivas Bharath7* Mitochondrial dysfunction and neurodegeneration underlie movement disorders such as Parkinson’s disease, Huntington’s disease and Manganism among others. As a corollary, inhibition of mitochondrial complex I (CI) and complex II (CII) by toxins 1‑methyl‑4‑phenylpyridinium (MPP+) and 3‑nitropropionic acid (3‑NPA) respectively, induced degenerative changes noted in such neurodegenerative diseases. We aimed to unravel the down‑stream pathways associated with CII inhibition and compared with CI inhibition and the Manganese (Mn) neurotoxicity. Genome‑wide transcriptomics of N27 neuronal cells exposed to 3‑NPA, compared with MPP+ and Mn revealed varied transcriptomic profle. Along with mitochondrial and synaptic pathways, Autophagy was the predominant pathway diferentially regulated in the 3‑NPA model with implications for neuronal survival. This pathway was unique to 3‑NPA, as substantiated by in silico modelling of the three toxins. Morphological and biochemical validation of autophagy markers in the cell model of 3‑NPA revealed incomplete autophagy mediated by mechanistic Target of Rapamycin Complex 2 (mTORC2) pathway. Interestingly, Brain Derived Neurotrophic Factor