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Titel:

The target landscape of clinical kinase drugs

Dokumenttyp:
Zeitschriftenaufsatz
Autor(en):
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...     »
Zeitschriftentitel:
Science
Jahr:
2017
Band / Volume:
358
Heft / Issue:
6367
Seitenangaben Beitrag:
eaan4368
Volltext / DOI:
doi:10.1126/science.aan4368
Verlag / Institution:
American Association for the Advancement of Science (AAAS)
E-ISSN:
0036-80751095-9203
Publikationsdatum:
30.11.2017
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