Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase

Title
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase
Authors
허우영Anastasia VelentzaSungjoon KimLaura FlatauerXinnong JiangDavid ValenteDaniel E. MasonMelissa SuzukiBrad LarsonJianming ZhangAnna ZagorskaMichael DiDonatoAdvait NagleMarkus WarmuthSteven P. BalkEric C. PetersNathanael S. Gray
Keywords
Irreversible inhibitors; Quinazoline scaffold; EFGR; Tec-family kinase; Bmx; Reactive cysteine
Issue Date
2008-07
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 18, 5916-5919
Abstract
Irreversible HER/erbB inhibitors selectively inhibit HER-family kinases by targeting a unique cysteine residue located within the ATP-binding pocket. Sequence alignment reveals that this rare cysteine is also present in ten other protein kinases including all five Tec-family members. We demonstrate that the Tec-family kinase Bmx is potently inhibited by irreversible modification at Cys496 by clinical stage EGFR inhibitors such as CI-1033. This cross-reactivity may have significant clinical implications.
URI
http://pubs.kist.re.kr/handle/201004/49746
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
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