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Document type:
Zeitschriftenaufsatz 
Author(s):
Heinzlmeir, Stephanie; Kudlinzki, Denis; Sreeramulu, Sridhar; Klaeger, Susan; Gande, Santosh Lakshmi; Linhard, Verena; Wilhelm, Mathias; Qiao, Huichao; Helm, Dominic; Ruprecht, Benjamin; Saxena, Krishna; Médard, Guillaume; Schwalbe, Harald; Kuster, Bernhard 
Title:
Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs 
Abstract:
The receptor tyrosine kinase EPHA2 (Ephrin type-A receptor 2) plays important roles in oncogenesis, metastasis, and treatment resistance, yet therapeutic targeting, drug discovery, or investigation of EPHA2 biology is hampered by the lack of appropriate inhibitors and structural information. Here, we used chemical proteomics to survey 235 clinical kinase inhibitors for their kinase selectivity and identified 24 drugs with submicromolar affinities for EPHA2. NMR-based conformational dynamics toge...    »
 
Journal title:
ACS Chemical Biology 
Year:
2016 
Journal volume:
11 
Journal issue:
12 
Pages contribution:
3400-3411 
Publisher:
American Chemical Society (ACS) 
E-ISSN:
1554-89291554-8937 
Date of publication:
07.11.2016