Probe Compound for Detecting and Isolating Enzymes and Means and Methods Using the Same
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Analgesics - antipyretics = „weak“ analgesics = non-opioid analgesics Most of them also • non-steroidal anti-inflamatory drugs (NSAIDs) •antirheumatics Oldřich Farsa 2011 Metabolism of eicosanoids O O arachidonic O H acid = 2 C O R1 R2 OH R2 O OH CH C O P O + 3 H N CH 2 O 3 CH3 glucocorticoids inhibitors of phspholipase A2 prostaglandins sythesis = COOH = "weak" analgesics + lipoxygenase inhibitors + NSAIDs arachidonic acid cyclooxygenases (COX1 + COX2) lipoxygenase OOH O COOH COOH O PG 5-hydroperoxy-6-trans-8,11,14-cis-eikosatetraenoic acid G2 OOH (5-HPETE) cyklooxygenases tromboxan synthase prostacyklin synthase PG H2 PG I2 = prostacyklin TX A2 endothelium cells LT A4 trombocytes isomerases PG D2 PG E2 LT C4 LT B4 PG F2α all the cells LT D4 LT E4 Effects of prostaglandins ↓ Prostaglandin E, F2α : ache, fewer, inflammation, sekretion of HCl , stomach mucosa capilaries dilatation, contraction of + ↑ uterus, kidneys: excretion of Na and H2O Prostacyclin (prostaglandin I ): vasodilatation, platelets aggregation inhibition 2 Tromboxan: vasokonstriction, platelets aggregation activation Leukotriens: alergic reactions (e.g. asthma bronchiale) Cyklooxygenases (= prostaglandin G/H synthases) COX1 Constitutive: in all the tissues Functions: •protection of stomach mucosa (vasodilatation) •diuresis •platelets aggregation (TXA) COX2 Philipp Needlemann Constitutive: kidneys, brain (co-localized with cyclins D and E) inventor of COX 1 isoenzymes Inducible: macrophages, neutrophfils, fibroblasts, endothelium cells (1989) Functions: •vasodilatation -
ATP-Citrate Lyase Has an Essential Role in Cytosolic Acetyl-Coa Production in Arabidopsis Beth Leann Fatland Iowa State University
Iowa State University Capstones, Theses and Retrospective Theses and Dissertations Dissertations 2002 ATP-citrate lyase has an essential role in cytosolic acetyl-CoA production in Arabidopsis Beth LeAnn Fatland Iowa State University Follow this and additional works at: https://lib.dr.iastate.edu/rtd Part of the Molecular Biology Commons, and the Plant Sciences Commons Recommended Citation Fatland, Beth LeAnn, "ATP-citrate lyase has an essential role in cytosolic acetyl-CoA production in Arabidopsis " (2002). Retrospective Theses and Dissertations. 1218. https://lib.dr.iastate.edu/rtd/1218 This Dissertation is brought to you for free and open access by the Iowa State University Capstones, Theses and Dissertations at Iowa State University Digital Repository. It has been accepted for inclusion in Retrospective Theses and Dissertations by an authorized administrator of Iowa State University Digital Repository. For more information, please contact [email protected]. ATP-citrate lyase has an essential role in cytosolic acetyl-CoA production in Arabidopsis by Beth LeAnn Fatland A dissertation submitted to the graduate faculty in partial fulfillment of the requirements for the degree of DOCTOR OF PHILOSOPHY Major: Plant Physiology Program of Study Committee: Eve Syrkin Wurtele (Major Professor) James Colbert Harry Homer Basil Nikolau Martin Spalding Iowa State University Ames, Iowa 2002 UMI Number: 3158393 INFORMATION TO USERS The quality of this reproduction is dependent upon the quality of the copy submitted. Broken or indistinct print, colored or poor quality illustrations and photographs, print bleed-through, substandard margins, and improper alignment can adversely affect reproduction. In the unlikely event that the author did not send a complete manuscript and there are missing pages, these will be noted. -
(12) Patent Application Publication (10) Pub. No.: US 2009/0156582 A1 Tsukamoto Et Al
US 20090156582A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2009/0156582 A1 Tsukamoto et al. (43) Pub. Date: Jun. 18, 2009 (54) PYRAZOLE COMPOUND Publication Classification (76) Inventors: Tetsuya Tsukamoto, Osaka-shi, (51) Int. Cl. Osaka (JP); Takeshi Yamamoto, A6II 3/55 (2006.01) Osaka-shi,Osaka (JP); Ryosuke A63L/454 (2006.01) Tokunoh, Osaka-shi, Osaka (JP); A63L/462 (2006.01) Tomohiro Kawamoto, Osaka-shi, C07D 403/02 (2006.01) Osaka (JP); Masahiro Okura, Osaka-shi, Osaka (JP); Masakumi (52) U.S. Cl. .................... 514/217.09: 514/406; 514/326; Kori, Osaka-shi, Osaka (JP); 548/364.1: 548/368.4: 546/211; 540/603 Katsuhito Murase, Osaka-shi, Osaka (JP) (57) ABSTRACT Correspondence Address: The present invention provides a pyrazole compound repre WENDEROTH, LIND & PONACK, L.L.P. sented by the formula (I): 1030 15th Street, N.W., Suite 400 East Washington, DC 20005-1503 (US) b (Io) (21) Appl. No.: 11/884,054 Ra R (22) PCT Filed: Feb. 9, 2006 (86). PCT No.: PCT/UP2006/302686 S371 (c)(1), wherein ring Ao is a pyrazole ring optionally further having 1 (2), (4) Date: Sep. 14, 2007 or 2 substituents; R is a substituted carbamoyl group; and R' (30) Foreign Application Priority Data is an optionally Substituted acylamino group, or a salt thereof or a prodrug thereof, which is useful as an agent for the Feb. 9, 2005 (JP) .................................. O333562005 prophylaxis or treatment of GSK-3? related pathology or Dec. 22, 2005 (JP) .................................. 3709622005 disease, and a GSK-3? inhibitor including same. US 2009/0156582 A1 Jun. -
Sleason, Redwood City, CA (US), Juan W. W333. a 3. C
USOO8288373B2 (12) United States Patent (10) Patent No.: US 8,288,373 B2 Chen et al. (45) Date of Patent: Oct. 16, 2012 (54) MODULATORS OF CXCR7 FOREIGN PATENT DOCUMENTS AU 2006-230674 A1 11, 2006 (75) Inventors: Xi Chen, Palo Alto, CA (US); Pingchen WO WOO2,08221 A2 1, 2002 Fan, Fremont, CA (US); Mark M. WO WOO3,O764OO A1 9, 2003 Sleason, Redwood City, CA (US), Juan W. W333. A 3. C. Jaen, Burlingame, CA (US). Lianfa WO WO 2007/126935 A2 11/2007 Li, Palo Alto, CA (US); Jeffrey P. WO WO 2008/008518 A1 1/2008 McMahon, Mountain View, CA (US); WO 2008, 11215.6 A1 9, 2008 Jay Powers, Pacifica, CA (US); Yibin Zeng, Foster City, CA (US); Penglie OTHER PUBLICATIONS Zhang, Foster City, CA (US) Konishi et al. (Yakugaku Zasshi (1973), 93(5), 684-7). Abstract.* r Miao et al., “CXCR7 (RDC1) promotes breast and lung tumor growth (73) Assignee: Chemocentryx, Inc., Mountain View, in vivo and is expressed on tumor-associated vasculature.” 2007. CA (US) PNAS, vol. 104. No. 40, pp. 15735-15740. c Zabel et al., “Elucidation of CXCR-7-Mediated Signaling Events and (*) Notice: Subject to any disclaimer the term of this Inhibition of CXCR4-Mediated Tumor Cell Transendothelial Migra patent is extended or adjusted under 35 tion by CXCR7 Ligands.” The Journal of Immunology, 2009, vol. U.S.C. 154(b) by 171 days. 183, Issue 5, pp. 3204-3211. International Search Reportmailed on Jan. 27, 2010, for International (21) Appl. No.: 12/612,638 Application No. PCT/US09/63298 filed on Nov. -
Etats Rapides
List of European Pharmacopoeia Reference Standards Effective from 2015/12/24 Order Reference Standard Batch n° Quantity Sale Information Monograph Leaflet Storage Price Code per vial Unit Y0001756 Exemestane for system suitability 1 10 mg 1 2766 Yes +5°C ± 3°C 79 ! Y0001561 Abacavir sulfate 1 20 mg 1 2589 Yes +5°C ± 3°C 79 ! Y0001552 Abacavir for peak identification 1 10 mg 1 2589 Yes +5°C ± 3°C 79 ! Y0001551 Abacavir for system suitability 1 10 mg 1 2589 Yes +5°C ± 3°C 79 ! Y0000055 Acamprosate calcium - reference spectrum 1 n/a 1 1585 79 ! Y0000116 Acamprosate impurity A 1 50 mg 1 3-aminopropane-1-sulphonic acid 1585 Yes +5°C ± 3°C 79 ! Y0000500 Acarbose 3 100 mg 1 See leaflet ; Batch 2 is valid until 31 August 2015 2089 Yes +5°C ± 3°C 79 ! Y0000354 Acarbose for identification 1 10 mg 1 2089 Yes +5°C ± 3°C 79 ! Y0000427 Acarbose for peak identification 3 20 mg 1 Batch 2 is valid until 31 January 2015 2089 Yes +5°C ± 3°C 79 ! A0040000 Acebutolol hydrochloride 1 50 mg 1 0871 Yes +5°C ± 3°C 79 ! Y0000359 Acebutolol impurity B 2 10 mg 1 -[3-acetyl-4-[(2RS)-2-hydroxy-3-[(1-methylethyl)amino] propoxy]phenyl] 0871 Yes +5°C ± 3°C 79 ! acetamide (diacetolol) Y0000127 Acebutolol impurity C 1 20 mg 1 N-(3-acetyl-4-hydroxyphenyl)butanamide 0871 Yes +5°C ± 3°C 79 ! Y0000128 Acebutolol impurity I 2 0.004 mg 1 N-[3-acetyl-4-[(2RS)-3-(ethylamino)-2-hydroxypropoxy]phenyl] 0871 Yes +5°C ± 3°C 79 ! butanamide Y0000056 Aceclofenac - reference spectrum 1 n/a 1 1281 79 ! Y0000085 Aceclofenac impurity F 2 15 mg 1 benzyl[[[2-[(2,6-dichlorophenyl)amino]phenyl]acetyl]oxy]acetate -
Expanding the Modular Ester Fermentative Pathways for Combinatorial Biosynthesis of Esters from Volatile Organic Acids
ARTICLE Expanding the Modular Ester Fermentative Pathways for Combinatorial Biosynthesis of Esters From Volatile Organic Acids Donovan S. Layton,1,2 Cong T. Trinh1,2,3 1 Department of Chemical and Biomolecular Engineering, University of Tennessee, Knoxville, Tennessee 2 BioEnergy Science Center (BESC), Oak Ridge National Laboratory, Oak Ridge, Tennessee 3 Bredesen Center for Interdisciplinary Research and Graduate Education, University of Tennessee, Knoxville, Tennessee; telephone: þ865-974-8121; fax: 865-974-7076; e-mail: [email protected] Biotechnol. Bioeng. 2016;113: 1764–1776. ABSTRACT: Volatile organic acids are byproducts of fermentative ß 2016 Wiley Periodicals, Inc. metabolism, for example, anaerobic digestion of lignocellulosic KEYWORDS: modular chassis cell; carboxylate; ester; acyl acetate; biomass or organic wastes, and are often times undesired inhibiting acyl acylate; ester fermentative pathway cell growth and reducing directed formation of the desired products. Here, we devised a general framework for upgrading these volatile organic acids to high-value esters that can be used as flavors, fragrances, solvents, and biofuels. This framework employs the acid-to-ester modules, consisting of an AAT (alcohol Introduction acyltransferase) plus ACT (acyl CoA transferase) submodule and an alcohol submodule, for co-fermentation of sugars and organic Harnessing renewable or waste feedstocks (e.g., switchgrass, corn acids to acyl CoAs and alcohols to form a combinatorial library of stover, agricultural residue, or municipal solid waste) -
Antagonists of Il-6 to Prevent Or Treat
(19) TZZ ¥_ _T (11) EP 2 376 126 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 39/00 (2006.01) C07K 16/24 (2006.01) 20.12.2017 Bulletin 2017/51 (86) International application number: (21) Application number: 09830695.4 PCT/US2009/006266 (22) Date of filing: 24.11.2009 (87) International publication number: WO 2010/065077 (10.06.2010 Gazette 2010/23) (54) ANTAGONISTS OF IL-6 TO PREVENT OR TREAT THROMBOSIS ANTAGONISTEN VON IL-6 ZUR PRÄVENTION ODER BEHANDLUNG VON THROMBOSE ANTAGONISTES D IL-6 POUR PRÉVENIR OU TRAITER LA THROMBOSE (84) Designated Contracting States: • MATSUYAMA MASASHI ET AL: AT BE BG CH CY CZ DE DK EE ES FI FR GB GR "Anti-interleukin-6 receptor antibody HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL (tocilizumab) treatment of multicentric PT RO SE SI SK SM TR Castleman’s disease", INTERNAL MEDICINE, JAPANESE SOCIETY OF INTERNAL MEDICINE, (30) Priority: 05.02.2009 US 366567 TOKYO, JP; BIOSCIENCES INFORMATION 14.07.2009 US 502581 SERVICE, PHILADELPHIA, PA, US, vol. 46, 1 25.11.2008 US 117811 P January 2007 (2007-01-01), pages 771-774, 25.11.2008 US 117861 P XP002696891, ISSN: 0918-2918, DOI: 24.02.2009 US 391717 10.2169/INTERNALMEDICINE.46.6262 06.03.2009 US 399156 • EMILLE D ET AL: "ADMINISTRATION OF AN 25.11.2008 US 117839 P ANTI-INTERLEUKIN-6 MONOCLONAL 24.02.2009 US 391615 ANTIBODY TO PATIENTS WITH ACQUIRED IMUNODEFICIENCY SYNDROME AND (43) Date of publication of application: LYMPHOMA: EFFECT ON LYMPHOMA GROWTH 19.10.2011 Bulletin 2011/42 AND ON B CLINICAL SYMPTOMS", BLOOD, AMERICAN SOCIETY OFHEMATOLOGY, US, vol. -
Structural Basis for Human Sterol Isomerase in Cholesterol Biosynthesis and Multidrug Recognition
ARTICLE https://doi.org/10.1038/s41467-019-10279-w OPEN Structural basis for human sterol isomerase in cholesterol biosynthesis and multidrug recognition Tao Long 1, Abdirahman Hassan 1, Bonne M Thompson2, Jeffrey G McDonald1,2, Jiawei Wang3 & Xiaochun Li 1,4 3-β-hydroxysteroid-Δ8, Δ7-isomerase, known as Emopamil-Binding Protein (EBP), is an endoplasmic reticulum membrane protein involved in cholesterol biosynthesis, autophagy, 1234567890():,; oligodendrocyte formation. The mutation on EBP can cause Conradi-Hunermann syndrome, an inborn error. Interestingly, EBP binds an abundance of structurally diverse pharmacolo- gically active compounds, causing drug resistance. Here, we report two crystal structures of human EBP, one in complex with the anti-breast cancer drug tamoxifen and the other in complex with the cholesterol biosynthesis inhibitor U18666A. EBP adopts an unreported fold involving five transmembrane-helices (TMs) that creates a membrane cavity presenting a pharmacological binding site that accommodates multiple different ligands. The compounds exploit their positively-charged amine group to mimic the carbocationic sterol intermediate. Mutagenesis studies on specific residues abolish the isomerase activity and decrease the multidrug binding capacity. This work reveals the catalytic mechanism of EBP-mediated isomerization in cholesterol biosynthesis and how this protein may act as a multi-drug binder. 1 Department of Molecular Genetics, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA. 2 Center for Human Nutrition, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA. 3 State Key Laboratory of Membrane Biology, School of Life Sciences, Tsinghua University, Beijing 100084, China. 4 Department of Biophysics, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA. -
(12) United States Patent (10) Patent No.: US 7,906,307 B2 S0e Et Al
US007906307B2 (12) United States Patent (10) Patent No.: US 7,906,307 B2 S0e et al. (45) Date of Patent: Mar. 15, 2011 (54) VARIANT LIPIDACYLTRANSFERASES AND 4,683.202 A 7, 1987 Mullis METHODS OF MAKING 4,689,297 A 8, 1987 Good 4,707,291 A 11, 1987 Thom 4,707,364 A 11/1987 Barach (75) Inventors: Jorn Borch Soe, Tilst (DK); Jorn 4,708,876 A 1 1/1987 Yokoyama Dalgaard Mikkelson, Hvidovre (DK); 4,798,793 A 1/1989 Eigtved 4,808,417 A 2f1989 Masuda Arno de Kreij. Geneve (CH) 4,810,414 A 3/1989 Huge-Jensen 4,814,331 A 3, 1989 Kerkenaar (73) Assignee: Danisco A/S, Copenhagen (DK) 4,818,695 A 4/1989 Eigtved 4,826,767 A 5/1989 Hansen 4,865,866 A 9, 1989 Moore (*) Notice: Subject to any disclaimer, the term of this 4,904.483. A 2f1990 Christensen patent is extended or adjusted under 35 4,916,064 A 4, 1990 Derez U.S.C. 154(b) by 0 days. 5,112,624 A 5/1992 Johna 5,213,968 A 5, 1993 Castle 5,219,733 A 6/1993 Myojo (21) Appl. No.: 11/852,274 5,219,744 A 6/1993 Kurashige 5,232,846 A 8, 1993 Takeda (22) Filed: Sep. 7, 2007 5,264,367 A 11/1993 Aalrust (Continued) (65) Prior Publication Data US 2008/OO70287 A1 Mar. 20, 2008 FOREIGN PATENT DOCUMENTS AR 331094 2, 1995 Related U.S. Application Data (Continued) (63) Continuation-in-part of application No. -
(12) United States Patent (10) Patent No.: US 8,642,021 B2 Brautigam Et Al
USOO8642021B2 (12) United States Patent (10) Patent No.: US 8,642,021 B2 Brautigam et al. (45) Date of Patent: *Feb. 4, 2014 (54) CONDITIONING COMPOSITION FOR HAIR FOREIGN PATENT DOCUMENTS (75) Inventors: Ina Brautigam, Darmstadt (DE); Frank DE 2630560 1/1978 ............... A61K 7.48 EP O315541 5, 1989 ............... A61K 7.48 Hermes, Seeheim (DE) FR 241 1001 7, 1979 ............... A61K 700 JP O7327633. A * 12/1995 (73) Assignee: Kao Germany GmbH, Darmstadt (DE) WO WOOO28966 A1 * 5, 2000 WO WOO3,070208 A1 8/2003 ............. A61K 7,134 (*) Notice: Subject to any disclaimer, the term of this patent is extended or adjusted under 35 OTHER PUBLICATIONS U.S.C. 154(b) by 1520 days. Abstract Accession No. 2000:35.1345 from the CaPlus database on This patent is Subject to a terminal dis STN, the bibliography, abstract and indexing data for WO 200028966 claimer. A1, downloaded on Aug. 8, 2007, 2 pages.* Quest International: “Yogurtene” Cosmetic Ingredients (Jun. 2000) (21) Appl. No.: 11/001,840 pp. 1-17.* Machine translation of JP 07327633A dowloaded from the JPO Feb. (22) Filed: Dec. 2, 2004 14, 2012.* thehealthyeating.org website (www.healthyeating.org/Milk-Dairy/ (65) Prior Publication Data Nutrients-in-Milk-Cheese-Yogurt/Yogurt-Nutrition. aspx?Referer-dairycouncilofca (downloaded Feb. 28, 2013).* US 2005/O152863 A1 Jul. 14, 2005 Website: Clairol's Touch of Yoghurt Shampoo (http://brandfailures. (30) Foreign Application Priority Data blogspot.com/2006/12/other-famous-brand-idea-failures.html) downloaded Feb. 28, 2013).* Skin Deep website http://www.ewg.org/skindeepfingredient/ Dec. 5, 2003 (EP) ..................................... O3O27985 702759/GUAR HYDROXYPROPYLTRIMONIUM CHLO RIDE/downloaded Sep. -
(12)UK Patent Application (1S1GB ,„>2577037 ,,3,A 2577037
(12)UK Patent Application (1S1GB ,„>2577037 ,,3,A (43) Date of A Publication 18.03.2020 (21) Application No: 1812997.3 (51) INT CL: C12N 15/52 (2006.01) C12P 33/02 (2006.01) (22) Date of Filing: 09.08.2018 C12R 1/32 (2006.01) C12R 1/365 (2006.01) (56) Documents Cited: GB 2102429 A EP 3112472 A (71) Applicant(s): WO 2001/031050 A US 4345029 A Cambrex Karlskoga AB US 4320195 A (Incorporated in Sweden) Appl Environ Microbiol, published online 4 May 2018, S-691 85 Karlskoga, Sweden Liu et al, "Characterization and engineering of 3- ketosteroid 9a-hydroxylases in Mycobacterium Rijksuniversiteit Groningen neoarum ATCC 25795 for the development of (Incorporated in the Netherlands) androst-1,4- diene3,17-dione and 9a-hydroxy- Broerstraat 5, 9712 CP Groningen, Netherlands androst-4-ene-3,17-dione-producing strains" Appl Environ Microbiol, Vol 77 (2011), Wilbrink et al, (72) Inventor(s): "FadD19 of Rhodococcus rhodochrous DMS43269, a Jonathan Knight steroid-coenzyme A ligase essential for degradation Cecilia Kvarnstrom Branneby of C-24 branched sterol side chains", pp 4455-4464 Lubbert Dijkhuizen FEMS Microbiol Letts, Vol 205 (2001), van der Geize et Janet Maria Petrusma al, "Unmarked gene deletion mutagenesis of kstD, Laura Fernandez De Las Heras encoding 3-ketosteroid deltal-dehydrogenase, in Rhodococcus erythropolis SQ1 using sacB as a counter-selectable marker", pp 197-202 (74) Agent and/or Address for Service: J Steroid Biochem Mol Biol, Vol 172 (2017), Guevara Potter Clarkson LLP et al, "Functional characterization of 3-ketosteroid 9a- The -
Biocatalytic Synthesis of Flavor Ester “Pentyl Valerate” Using Candida Rugosa Lipase Immobilized in Microemulsion Based Organogels: Effect of Parameters and Reusability
Hindawi Publishing Corporation BioMed Research International Volume 2014, Article ID 353845, 14 pages http://dx.doi.org/10.1155/2014/353845 Research Article Biocatalytic Synthesis of Flavor Ester ‘‘Pentyl Valerate’’ Using Candida rugosa Lipase Immobilized in Microemulsion Based Organogels: Effect of Parameters and Reusability Tripti Raghavendra,1 Nilam Panchal,1 Jyoti Divecha,2 Amita Shah,1 and Datta Madamwar1 1 BRD School of Biosciences, Sardar Patel Maidan, Sardar Patel University, Satellite Campus, Vadtal Road, P.O. Box 39, Vallabh Vidyanagar, Gujarat 388120, India 2 Department of Statistics, Sardar Patel University, Vallabh Vidyanagar, Gujarat 388120, India Correspondence should be addressed to Datta Madamwar; datta [email protected] Received 28 February 2014; Revised 5 May 2014; Accepted 19 May 2014; Published 1 July 2014 Academic Editor: Yunjun Yan Copyright © 2014 Tripti Raghavendra et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. Pentyl valerate was synthesized biocatalytically using Candida rugosa lipase (CRL) immobilized in microemulsion based organogels ∘ (MBGs). The optimum conditions were found to be pH 7.0, temperature of 37 C, ratio of concentration of water to surfactant (Wo) of 60, and the surfactant sodium bis-2-(ethylhexyl)sulfosuccinate (AOT) for MBG preparation. Although kinetic studies revealed that the enzyme in free form had high affinity towards substrates ( = 23.2 mM for pentanol and 76.92 mM for valeric acid) whereas, after immobilization, the values increased considerably (74.07 mM for pentanol and 83.3 mM for valeric acid) resulting in a slower reaction rate, the maximum conversion was much higher in case of immobilized enzyme (∼99%) as compared to free enzyme (∼19%).