The target landscape of clinical kinase drugs

Klaeger, Susan; Heinzlmeir, Stephanie; Wilhelm, Mathias; Polzer, Harald; Vick, Binje; Koenig, Paul-Albert; Reinecke, Maria; Ruprecht, Benjamin; Petzoldt, Svenja; Meng, Chen; Zecha, Jana; Reiter, Katrin; Qiao, Huichao; Helm, Dominic; Koch, Heiner; Schoof, Melanie; Canevari, Giulia; Casale, Elena; Re Depaolini, Stefania; Feuchtinger, Annette; Wu, Zhixiang; Schmidt, Tobias; Rueckert, Lars; Becker, Wilhelm; Huenges, Jan; Garz, Anne-Kathrin; Gohlke, Björn-Oliver; P. Zolg, Daniel; Kayser, Gian; Vooder, Tõnu; Preißner, Robert; Hahne, Hannes; Tõnisson, Neeme; Kramer, Karl; S. Götze, Katharina; Bassermann, Florian; Schlegl, Judith; Ehrlich, Hans‐Christian; Aiche, Stephan; Walch, Axel; A. Greif, Philipp; Schneider, Sabine; Felder, Eduard; Ruland, Jürgen; Médard, Guillaume; Jeremias, Irmela; Spiekermann, Karsten; Küster, Bernhard

doi:10.1126/science.aan4368

Public

The target landscape of clinical kinase drugs

Published in Science • Nov 30, 2017

Authors:

Susan Klaeger

Stephanie Heinzlmeir

Mathias Wilhelm

Abstract

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 previousl...

Subject

Kinome

Druggability

Drug repositioning

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