The promise and peril of chemical probes

被引：603

作者：

Arrowsmith, Cheryl H. ^{[1
,2
]}

Audia, James E. ^{[3
]}

Austin, Christopher ^{[4
]}

Baell, Jonathan ^{[5
]}

Bennett, Jonathan ^{[6
]}

Blagg, Julian ^{[7
]}

Bountra, Chas ^{[8
]}

Brennan, Paul E. ^{[8
,9
]}

Brown, Peter J. ^{[1
]}

Bunnage, Mark E. ^{[10
]}

Buser-Doepner, Carolyn ^{[11
]}

Campbell, Robert M. ^{[12
]}

Carter, Adrian J. ^{[13
]}

Cohen, Philip ^{[14
]}

Copeland, Robert A. ^{[15
]}

Cravatt, Ben ^{[16
]}

Dahlin, Jayme L. ^{[17
]}

Dhanak, Dashyant ^{[18
]}

Edwards, Aled M. ^{[1
]}

Frye, Stephen V. ^{[19
]}

Gray, Nathanael ^{[20
]}

Grimshaw, Charles E. ^{[21
]}

Hepworth, David ^{[10
]}

Howe, Trevor ^{[22
]}

Huber, Kilian V. M. ^{[23
]}

Jin, Jian ^{[24
,25
,26
]}

Knapp, Stefan ^{[8
,9
]}

Kotz, Joanne D. ^{[27
]}

Kruger, Ryan G. ^{[28
]}

Lowe, Derek ^{[29
]}

Mader, Mary M. ^{[12
]}

Marsden, Brian ^{[8
]}

Mueller-Fahrnow, Anke ^{[30
]}

Mueller, Susanne ^{[8
,9
]}

O'Hagan, Ronan C. ^{[31
]}

Overington, John P. ^{[32
,33
]}

Owen, Dafydd R. ^{[10
]}

Rosenberg, Saul H. ^{[34
]}

Roth, Brian ^{[35
]}

Ross, Ruth ^{[36
]}

Schapira, Matthieu ^{[1
,36
]}

Schreiber, Stuart L. ^{[27
]}

Shoichet, Brian ^{[37
]}

Sundstrom, Michael ^{[38
,39
,40
]}

Superti-Furga, Giulio ^{[23
,41
]}

Taunton, Jack ^{[42
,43
]}

Toledo-Sherman, Leticia ^{[44
]}

Walpole, Chris ^{[45
]}

Walters, Michael A. ^{[46
]}

Willson, Timothy M. ^{[35
,47
]}

机构：

[1] Struct Genom Consortium, Toronto, ON, Canada

[2] Univ Toronto, Dept Med Biophys, Princess Margaret Canc Ctr, Toronto, ON, Canada

[3] Constellat Pharmaceut, Cambridge, MA USA

[4] NIH, Natl Ctr Adv Translat Sci, Bethesda, MD 20892 USA

[5] Monash Univ, Fac Pharm & Pharmaceut Sci, Melbourne, Vic 3004, Australia

[6] Merck Res Labs, Discovery Chem, Boston, MA USA

[7] Inst Canc Res, Canc Res UK Canc Therapeut Unit, London SW3 6JB, England

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

[9] Univ Oxford, Target Discovery Inst, Oxford, England

[10] Pfizer, Worldwide Med Chem, Cambridge, MA USA

[11] GlaxoSmithKline, Collegeville, PA USA

[12] Eli Lilly & Co, Lilly Res Labs, Indianapolis, IN 46285 USA

[13] Boehringer Ingelheim GmbH & Co KG, Corp Dept Res Networking, Ingelheim, Germany

[14] Univ Dundee, Sir James Black Ctr, Dundee, Scotland

[15] Epizyme Inc, Cambridge, MA USA

[16] Scripps Res Inst, Dept Physiol Chem, San Diego, CA USA

[17] Mayo Clin, Coll Med, Dept Mol Pharmacol & Expt Therapeut, Rochester, MN USA

[18] Janssen Res & Dev, Spring House, PA USA

[19] Univ N Carolina, Eshelman Sch Pharm, Ctr Integrat Chem Biol & Drug Discovery, Div Chem Biol & Med Chem, Chapel Hill, NC USA

[20] Harvard Univ, Dept Biol Chem & Mol Pharmacol, Cambridge, MA 02138 USA

[21] Takeda Calif Inc, San Diego, CA USA

[22] Janssen Res & Dev, High Wycombe, Bucks, England

[23] Austrian Acad Sci, CeMM Res Ctr Mol Med, A-1010 Vienna, Austria

[24] Icahn Sch Med Mt Sinai, Dept Struct & Chem Biol, New York, NY 10029 USA

[25] Icahn Sch Med Mt Sinai, Dept Oncol Sci, New York, NY 10029 USA

[26] Icahn Sch Med Mt Sinai, Dept Pharmacol & Syst Therapeut, New York, NY 10029 USA

[27] Broad Inst, Ctr Sci Therapeut, Cambridge, MA USA

[28] GlaxoSmithKline, Canc Epigenet, Collegeville, PA USA

[29] Vertex Pharmaceut, Boston, MA USA

[30] Bayer Pharma AG, Berlin, Germany

[31] Merck Res Labs, Oncol Discovery, Boston, MA USA

[32] European Bioinformat Inst, European Mol Biol Lab, Hinxton, England

[33] Stratified Med, London, England

[34] AbbVie, N Chicago, IL USA

[35] Univ N Carolina, Eshelman Sch Pharm, Chapel Hill, NC USA

[36] Univ Toronto, Dept Pharmacol & Toxicol, Toronto, ON, Canada

[37] Univ Calif San Francisco, Sch Pharm, San Francisco, CA 94143 USA

[38] Karolinska Inst, Struct Genom Consortium, Solna, Sweden

[39] Karolinska Univ Hosp, Dept Med, Solna, Sweden

[40] Karolinska Inst, Solna, Sweden

[41] Med Univ Vienna, Ctr Physiol & Pharmacol, Vienna, Austria

[42] Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA

[43] Univ Calif San Francisco, Howard Hughes Med Inst, San Francisco, CA USA

[44] CHDI Fdn, CHDI Management, Los Angeles, CA USA

[45] McGill Univ, Struct Genom Consortium, Montreal, PQ, Canada

[46] Univ Minnesota, Minneapolis, MN USA

[47] Univ N Carolina, Struct Genom Consortium, Chapel Hill, NC USA

[48] Simon Fraser Univ, Dept Chem, Burnaby, BC V5A 1S6, Canada

来源：

NATURE CHEMICAL BIOLOGY | 2015年 / 11卷 / 08期

基金：

英国惠康基金; 英国医学研究理事会;

关键词：

PROTEIN-KINASE; TARGET ENGAGEMENT; POTENT INHIBITOR; IDENTIFICATION; HYDROLASE; MECHANISM; AGONIST; CELLS;

D O I：

10.1038/nchembio.1867

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Chemical probes are powerful reagents with increasing impacts on biomedical research. However, probes of poor quality or that are used incorrectly generate misleading results. To help address these shortcomings, we will create a community-driven wiki resource to improve quality and convey current best practice.

引用

页码：536 / 541

页数：6

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