Seeding Collaborations to Advance Kinase Science with the GSK Published Kinase Inhibitor Set (PKIS)

被引：82

作者：

Drewry, David H. ^{[1
]}

Willson, Timothy M. ^{[1
]}

Zuercher, William J. ^{[1
]}

机构：

[1] GlaxoSmithKline, Dept Biol Chem, Res Triangle Pk, NC 27709 USA

来源：

CURRENT TOPICS IN MEDICINAL CHEMISTRY | 2014年 / 14卷 / 03期

关键词：

Open access chemical biology; kinase inhibitor probe; EPENDYMOMA; KINOME;

D O I：

10.2174/1568026613666131127160819

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

To catalyze research on historically untargeted protein kinases, we created the PKIS, an annotated set of 367 small molecule kinase inhibitors. The set has been widely distributed to academic collaborators as an open access tool. It has been used to identify chemical starting points for development of chemical probes for orphan kinases and to investigate kinase signaling in high content phenotypic assays. Access to the set comes with few restrictions other than the requirement that assay results be released into the public domain for the benefit of the entire research community. Examples from the efforts of several collaborators are summarized.

引用

页码：340 / 342

页数：3

共 13 条

[1] An Integrated In Vitro and In Vivo High-Throughput Screen Identifies Treatment Leads for Ependymoma [J].

Atkinson, Jennifer M. ;

Shelat, Anang A. ;

Carcaboso, Angel Montero ;

Kranenburg, Tanya A. ;

Arnold, Leggy A. ;

Boulos, Nidal ;

Wright, Karen ;

Johnson, Robert A. ;

Poppleton, Helen ;

Mohankumar, Kumarasamypet M. ;

Feau, Clementine ;

Phoenix, Timothy ;

Gibson, Paul ;

Zhu, Liqin ;

Tong, Yiai ;

Eden, Chris ;

Ellison, David W. ;

Priebe, Waldemar ;

Koul, Dimpy ;

Yung, W. K. Alfred ;

Gajjar, Amar ;

Stewart, Clinton F. ;

Guy, R. Kiplin ;

Gilbertson, Richard J. .

CANCER CELL, 2011, 20 (03) :384-399

[2] Target validation using chemical probes [J].

Bunnage, Mark E. ;

Chekler, Eugene L. Piatnitski ;

Jones, Lyn H. .

NATURE CHEMICAL BIOLOGY, 2013, 9 (04) :195-199

[3] Profile of the GSK Published Protein Kinase Inhibitor Set Across ATP-Dependent and-Independent Luciferases: Implications for Reporter-Gene Assays [J].

Dranchak, Patricia ;

MacArthur, Ryan ;

Guha, Rajarshi ;

Zuercher, William J. ;

Drewry, David H. ;

Auld, Douglas S. ;

Inglese, James .

PLOS ONE, 2013, 8 (03)

[4] Too many roads not taken [J].

Edwards, Aled M. ;

Isserlin, Ruth ;

Bader, Gary D. ;

Frye, Stephen V. ;

Willson, Timothy M. ;

Yu, Frank H. .

NATURE, 2011, 470 (7333) :163-165

[5] The (un)targeted cancer kinome [J].

Fedorov, Oleg ;

Mueller, Susanne ;

Knapp, Stefan .

NATURE CHEMICAL BIOLOGY, 2010, 6 (03) :166-169

[6] Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit [J].

Fish, Paul V. ;

Filippakopoulos, Panagis ;

Bish, Gerwyn ;

Brennan, Paul E. ;

Bunnage, Mark E. ;

Cook, Andrew S. ;

Federov, Oleg ;

Gerstenberger, Brian S. ;

Jones, Hannah ;

Knapp, Stefan ;

Marsden, Brian ;

Nocka, Karl ;

Owen, Dafydd R. ;

Philpott, Martin ;

Picaud, Sarah ;

Primiano, Michael J. ;

Ralph, Michael J. ;

Sciammetta, Nunzio ;

Trzupek, John D. .

JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (22) :9831-9837

[7] ChEMBL: a large-scale bioactivity database for drug discovery [J].

Gaulton, Anna ;

Bellis, Louisa J. ;

Bento, A. Patricia ;

Chambers, Jon ;

Davies, Mark ;

Hersey, Anne ;

Light, Yvonne ;

McGlinchey, Shaun ;

Michalovich, David ;

Al-Lazikani, Bissan ;

Overington, John P. .

NUCLEIC ACIDS RESEARCH, 2012, 40 (D1) :D1100-D1107

[8] Cross-species genomics matches driver mutations and cell compartments to model ependymoma [J].

Johnson, Robert A. ;

Wright, Karen D. ;

Poppleton, Helen ;

Mohankumar, Kumarasamypet M. ;

Finkelstein, David ;

Pounds, Stanley B. ;

Rand, Vikki ;

Leary, Sarah E. S. ;

White, Elsie ;

Eden, Christopher ;

Hogg, Twala ;

Northcott, Paul ;

Mack, Stephen ;

Neale, Geoffrey ;

Wang, Yong-Dong ;

Coyle, Beth ;

Atkinson, Jennifer ;

DeWire, Mariko ;

Kranenburg, Tanya A. ;

Gillespie, Yancey ;

Allen, Jeffrey C. ;

Merchant, Thomas ;

Boop, Fredrick A. ;

Sanford, Robert. A. ;

Gajjar, Amar ;

Ellison, David W. ;

Taylor, Michael D. ;

Grundy, Richard G. ;

Gilbertson, Richard J. .

NATURE, 2010, 466 (7306) :632-636

[9] A public-private partnership to unlock the untargeted kinome [J].

Knapp, Stefan ;

Arruda, Paulo ;

Blagg, Julian ;

Burley, Stephen ;

Drewry, David H. ;

Edwards, Aled ;

Fabbro, Doriano ;

Gillespie, Paul ;

Gray, Nathanael S. ;

Kuster, Bernhard ;

Lackey, Karen E. ;

Mazzafera, Paulo ;

Tomkinson, Nicholas C. O. ;

Willson, Timothy M. ;

Workman, Paul ;

Zuercher, William J. .

NATURE CHEMICAL BIOLOGY, 2013, 9 (01) :3-7

[10] Small-Molecule Inhibition of BRDT for Male Contraception [J].

Matzuk, Martin M. ;

McKeown, Michael R. ;

Filippakopoulos, Panagis ;

Li, Qinglei ;

Ma, Lang ;

Agno, Julio E. ;

Lemieux, Madeleine E. ;

Picaud, Sarah ;

Yu, Richard N. ;

Qi, Jun ;

Knapp, Stefan ;

Bradner, James E. .

CELL, 2012, 150 (04) :673-684

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