Proteomics

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Target Landscape of Clinical Kinase Inhibitors

ABSTRACT: Here, we provide a comprehensive overview of the selectivity profiles of 242 kinase inhibitors currently in clinical trials. We screened available inhibitors against human protein kinases by using the Kinobead technology resulting in a drug matrix identifying the druggable kinome and related proteins.

INSTRUMENT(S): Orbitrap Fusion, Q Exactive HF, LTQ Orbitrap Elite, Q Exactive

ORGANISM(S): Homo Sapiens (human)

SUBMITTER: Susan Klaeger  

LAB HEAD: Bernhard Kuster

PROVIDER: PXD005336 | Pride | 2017-12-01

REPOSITORIES: Pride

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The target landscape of clinical kinase drugs.

Klaeger Susan S   Heinzlmeir Stephanie S   Wilhelm Mathias M   Polzer Harald H   Vick Binje B   Koenig Paul-Albert PA   Reinecke Maria M   Ruprecht Benjamin B   Petzoldt Svenja S   Meng Chen C   Zecha Jana J   Reiter Katrin K   Qiao Huichao H   Helm Dominic D   Koch Heiner H   Schoof Melanie M   Canevari Giulia G   Casale Elena E   Depaolini Stefania Re SR   Feuchtinger Annette A   Wu Zhixiang Z   Schmidt Tobias T   Rueckert Lars L   Becker Wilhelm W   Huenges Jan J   Garz Anne-Kathrin AK   Gohlke Bjoern-Oliver BO   Zolg Daniel Paul DP   Kayser Gian G   Vooder Tonu T   Preissner Robert R   Hahne Hannes H   Tõnisson Neeme N   Kramer Karl K   Götze Katharina K   Bassermann Florian F   Schlegl Judith J   Ehrlich Hans-Christian HC   Aiche Stephan S   Walch Axel A   Greif Philipp A PA   Schneider Sabine S   Felder Eduard Rudolf ER   Ruland Juergen J   Médard Guillaume G   Jeremias Irmela I   Spiekermann Karsten K   Kuster Bernhard B  

Science (New York, N.Y.) 20171201 6367

Kinase inhibitors are important cancer therapeutics. Polypharmacology is commonly observed, requiring thorough target deconvolution to understand drug mechanism of action. Using chemical proteomics, we analyzed the target spectrum of 243 clinically evaluated kinase drugs. The data revealed previously unknown targets for established drugs, offered a perspective on the "druggable" kinome, highlighted (non)kinase off-targets, and suggested potential therapeutic applications. Integration of phosphop  ...[more]

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