Discovery of a Selective Irreversible BMX Inhibitor for Prostate Cancer

Title
Discovery of a Selective Irreversible BMX Inhibitor for Prostate Cancer
Authors
Feiyang LiuXin ZhangEllen WeisbergSen Chen허우영Hong WuZheng ZhaoWenchao WangMao MaoChangmeng CaiNicholas I. SimonTakaomi SandaJinhua WangA. Thomas LookJames D. GriffinSteven P. BalkQingsong LiuNathanael S. Gray
Issue Date
2013-04
Publisher
ACS Chemical Biology
Citation
VOL 8, NO 7, 1423-1428
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.
URI
http://pubs.kist.re.kr/handle/201004/49734
ISSN
15548929
Appears in Collections:
KIST Publication > Article
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