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Title:

Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs

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
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
Fulltext / DOI:
doi:10.1021/acschembio.6b00709
Publisher:
American Chemical Society (ACS)
E-ISSN:
1554-89291554-8937
Date of publication:
07.11.2016
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