Get started
Work

Discovery of a Selective Irreversible BMX Inhibitor for Prostate Cancer

Year: 2013
Type: article
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.
DOI: 10.1021/cb4000629
Authors: Feiyang Liu, 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
Language: English
Field: Chemistry
Open Access status: green
OpenAlex ID: W2070188918
FWCI: 1.958
Cites: 16
Cited by: 52
Related to: 10