Occupational hazards: allosteric regulation of protein kinases through the nucleotide-binding pocket

被引：4

作者：

Cameron, Angus J. M. ^{[1
]}

机构：

[1] Canc Res UK, London Res Inst, London WC2A 3LY, England

来源：

BIOCHEMICAL SOCIETY TRANSACTIONS | 2011年 / 39卷

关键词：

allosteric regulation; mammalian target of rapamycin (mTOR); nucleotide-binding pocket; protein kinase C (PKC); WILD-TYPE; INHIBITORS; RAF; BRAF; ACTIVATION; MUTANTS; YEAST; PDK1; KIT; ABL;

D O I：

10.1042/BST0390472

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

Targeting the protein kinase ATP-binding pocket provides a significant opportunity for the treatment of disease. Recent studies have revealed a central activity-independent role for nucleotide pocket occupation in the allosteric behaviour of diverse kinases. Regulation of nucleotide pocket conformation with either nucleotides or ATP competitive inhibitors has revealed an added dimension to the targeting of kinases. In the present paper, using PKC (protein kinase C) as a paradigm, the liabilities and opportunities associated with the occupation of the nucleotide pocket are explored.

引用

页码：472 / 476

页数：5

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