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Titel:

The target landscape of clinical kinase drugs.

Dokumenttyp:
Journal Article; Research Support, Non-U.S. Gov't; Article
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
Sprache:
eng
Volltext / DOI:
doi:10.1126/science.aan4368
PubMed:
http://view.ncbi.nlm.nih.gov/pubmed/29191878
Print-ISSN:
0036-8075
TUM Einrichtung:
III. Medizinische Klinik und Poliklinik (Hämatologie / Onkologie); Institut für Klinische Chemie und Pathobiochemie
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