Inhibitors paradoxically prime kinases

被引：12

作者：

Frye, Stephen V. ^{[1
,2
]}

Johnson, Gary L. ^{[3
]}

机构：

[1] Univ N Carolina, Div Med Chem & Nat Prod, Eshelman Sch Pharm, Chapel Hill, NC 27515 USA

[2] Univ N Carolina, Ctr Integrat Chem Biol & Drug Discovery, Chapel Hill, NC USA

[3] Univ N Carolina, Dept Pharmacol, Chapel Hill, NC USA

来源：

NATURE CHEMICAL BIOLOGY | 2009年 / 5卷 / 07期

关键词：

PROTEIN-KINASE; AKT; SELECTIVITY;

D O I：

10.1038/nchembio.f.11

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Small-molecule inhibitors can induce phosphorylation priming of AGC kinases. Priming by ATP binding pocket conformation, rather than intrinsic kinase activity, has significant implications for drug discovery and therapeutic efficacy.

引用

页码：448 / 449

页数：2

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