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Title:

The target landscape of clinical kinase drugs.

Document type:
Journal Article; Research Support, Non-U.S. Gov't; Article
Author(s):
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; Depaolini, Stefania Re; Feuchtinger, Annette; Wu, Zhixiang; Schmidt, Tobias; Rueckert, Lars; Becker, Wilhelm; Huenges, Jan; Garz, Anne-Kathrin; Gohlke, Bjoern-Oliver; Zolg, Daniel Paul; Kayser, Gian; Voo...     »
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 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...     »
Journal title abbreviation:
Science
Year:
2017
Journal volume:
358
Journal issue:
6367
Language:
eng
Fulltext / DOI:
doi:10.1126/science.aan4368
Pubmed ID:
http://view.ncbi.nlm.nih.gov/pubmed/29191878
Print-ISSN:
0036-8075
TUM Institution:
III. Medizinische Klinik und Poliklinik (Hämatologie / Onkologie); Institut für Klinische Chemie und Pathobiochemie
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