Progress towards a public chemogenomic set for protein kinases and a call for contributions

被引：105

作者：

Drewry, David H. ^{[1
]}

Wells, Carrow I. ^{[1
]}

Andrews, David M. ^{[2
]}

Angell, Richard ^{[3
]}

Al-Ali, Hassan ^{[4
,5
]}

Axtman, Alison D. ^{[1
]}

Capuzzi, Stephen J. ^{[6
]}

Elkins, Jonathan M. ^{[7
]}

Ettmayer, Peter ^{[8
]}

Frederiksen, Mathias ^{[9
]}

Gileadi, Opher ^{[10
,11
]}

Gray, Nathanael ^{[12
,13
]}

Hooper, Alice ^{[3
]}

Knapp, Stefan ^{[14
,15
]}

Laufer, Stefan ^{[16
]}

Luecking, Ulrich ^{[17
]}

Michaelides, Michael ^{[18
]}

Mueller, Susanne ^{[14
,15
]}

Muratov, Eugene ^{[6
]}

Denny, R. Aldrin ^{[19
]}

Saikatendu, Kumar S. ^{[20
]}

Treiber, Daniel K. ^{[21
]}

Zuercher, William J. ^{[1
]}

Willson, Timothy M. ^{[1
]}

机构：

[1] Univ North Carolina Chapel Hill, Struct Genom Consortium, UNC Eshelman Sch Pharm, Chapel Hill, NC 27599 USA

[2] AstraZeneca, Darwin Bldg,Cambridge Sci Pk, Cambridge, England

[3] UCL, Sch Pharm, Drug Discovery Grp, Translat Res Off, 29-39 Brunswick Sq, London, England

[4] Univ Miami, Miller Sch Med, Miami Project Cure Paralysis, Miami, FL 33136 USA

[5] Univ Miami, Miller Sch Med, Peggy & Harold Katz Family Drug Discovery Ctr, Miami, FL 33136 USA

[6] Univ North Carolina Chapel Hill Chapel, Lab Mol Modeling, Div Chem Biol & Med Chem, UNC Eshelman Sch Pharm, Chapel Hill, NC USA

[7] Univ Estadual Campinas UNICAMP, Struct Genom Consortium, Campinas, SP, Brazil

[8] Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria

[9] Novartis Inst BioMed Res, Novartis Campus, Basel, Switzerland

[10] Univ Oxford, Struct Genom Consortium, Oxford, England

[11] Univ Oxford, Nuffield Dept Clin Med, Target Discovery Inst, Oxford, England

[12] Harvard Med Sch, Harvard Dept Biol Chem & Mol Pharmacol, Boston, MA USA

[13] Dana Farber Canc Inst, Dept Canc Biol, Boston, MA 02115 USA

[14] Goethe Univ Frankfurt, Struct Genom Consortium, Buchmann Inst Mol Life Sci, Max von Laue Str 15, Frankfurt, Germany

[15] Goethe Univ Frankfurt, Inst Pharmaceut Chem, Max von Laue Str 15, Frankfurt, Germany

[16] Eberhard Karls Univ Tubingen, Dept Pharmaceut Chem, Inst Pharmaceut Sci, Morgenstelle 8, Tubingen, Germany

[17] Bayer Pharma AG, Drug Discovery, Mullerstr 178, Berlin, Germany

[18] AbbVie, Oncol Chem, 1 North Waukegan Rd, N Chicago, IL USA

[19] Pfizer Inc, Worldwide Med Chem, Cambridge, MA USA

[20] Takeda Calif Inc, Global Res Externalizat, 10410 Sci Ctr Dr, San Diego, CA USA

[21] DiscoverX Corp, Fremont, CA USA

来源：

PLOS ONE | 2017年 / 12卷 / 08期

基金：

加拿大创新基金会; 巴西圣保罗研究基金会; 英国惠康基金;

关键词：

CANCER-CELLS; INHIBITOR; IDENTIFICATION; INTERROGATION; SENSITIVITY; SELECTIVITY; DEPENDENCY; TARGETS;

D O I：

10.1371/journal.pone.0181585

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

Protein kinases are highly tractable targets for drug discovery. However, the biological function and therapeutic potential of the majority of the 500+ human protein kinases remains unknown. We have developed physical and virtual collections of small molecule inhibitors, which we call chemogenomic sets, that are designed to inhibit the catalytic function of almost half the human protein kinases. In this manuscript we share our progress towards generation of a comprehensive kinase chemogenomic set (KCGS), release kinome profiling data of a large inhibitor set (Published Kinase Inhibitor Set 2 (PKIS2)), and outline a process through which the community can openly collaborate to create a KCGS that probes the full complement of human protein kinases.

引用

页数：20

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