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dc.contributor.authorFeiyang Liu-
dc.contributor.authorXin Zhang-
dc.contributor.authorEllen Weisberg-
dc.contributor.authorSen Chen-
dc.contributor.author허우영-
dc.contributor.authorHong Wu-
dc.contributor.authorZheng Zhao-
dc.contributor.authorWenchao Wang-
dc.contributor.authorMao Mao-
dc.contributor.authorChangmeng Cai-
dc.contributor.authorNicholas I. Simon-
dc.contributor.authorTakaomi Sanda-
dc.contributor.authorJinhua Wang-
dc.contributor.authorA. Thomas Look-
dc.contributor.authorJames D. Griffin-
dc.contributor.authorSteven P. Balk-
dc.contributor.authorQingsong Liu-
dc.contributor.authorNathanael S. Gray-
dc.date.accessioned2015-12-03T02:03:05Z-
dc.date.available2015-12-03T02:03:05Z-
dc.date.issued201304-
dc.identifier.citationVOL 8, NO 7, 1423-1428-
dc.identifier.issn15548929-
dc.identifier.other44315-
dc.identifier.urihttp://pubs.kist.re.kr/handle/201004/49734-
dc.description.abstractBMX 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.-
dc.publisherACS Chemical Biology-
dc.titleDiscovery of a Selective Irreversible BMX Inhibitor for Prostate Cancer-
dc.typeArticle-
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