| Literature DB >> 23594111 |
Feiyang Liu1, Xin Zhang, Ellen Weisberg, Sen Chen, Wooyoung Hur, Hong Wu, Zheng Zhao, Wenchao Wang, Mao Mao, Changmeng Cai, Nicholas I Simon, Takaomi Sanda, Jinhua Wang, A Thomas Look, James D Griffin, Steven P Balk, Qingsong Liu, Nathanael S Gray.
Abstract
BMX is a member of the TEC family of nonreceptor tyrosine kinases. We have used structure-based drug design in conjunction with kinome profiling to develop a potent, selective, and irreversible BMX kinase inhibitor, BMX-IN-1, which covalently modifies Cys496. BMX-IN-1 inhibits the proliferation of Tel-BMX-transformed Ba/F3 cells at two digit nanomolar concentrations but requires single digit micromolar concentrations to inhibit the proliferation of prostate cancer cell lines. Using a combinatorial kinase inhibitor screening strategy, we discovered that the allosteric Akt inhibitor, MK2206, is able to potentiate BMX inhibitor's antiproliferation efficacy against prostate cancer cells.Entities:
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Year: 2013 PMID： 23594111 DOI： 10.1021/cb4000629
Source DB: PubMed Journal: ACS Chem Biol ISSN： 1554-8929 Impact factor: 5.100