Protein kinase C intervention-the state of play

被引：81

作者：

Roffey, Jon ^{[2
]}

Rosse, Carine ^{[1
]}

Linch, Mark ^{[1
]}

Hibbert, Andrew ^{[1
]}

McDonald, Neil Q. ^{[3
]}

Parker, Peter J. ^{[1
,4
]}

机构：

[1] London Res Inst, Lincolns Inn Fields Labs, Prot Phosphorylat Lab, London WC2A 3PX, England

[2] Canc Res Technol Ltd, Wolfson Inst Biomed Res, Discovery Lab, London WC1E 6BT, England

[3] London Res Inst, Lincolns Inn Fields Labs, Struct Biol Lab, London WC2A 3PX, England

[4] Kings Coll London, Guys Hosp, Sect Canc Cell Biol & Imaging, Div Canc Studies, London SE1 1UL, England

来源：

CURRENT OPINION IN CELL BIOLOGY | 2009年 / 21卷 / 02期

关键词：

GASTROINTESTINAL STROMAL TUMORS; SPINOCEREBELLAR ATAXIA TYPE-14; ISCHEMIA-REPERFUSION INJURY; NON-HODGKINS-LYMPHOMA; ALPHA MESSENGER-RNA; LUNG-CANCER CELLS; DELTA-NULL MICE; PKC-THETA; DOWN-REGULATION; SELECTIVE INHIBITORS;

D O I：

10.1016/j.ceb.2009.01.019

中图分类号：

Q2 [细胞生物学];

学科分类号：

071009 ; 090102 ;

摘要：

Intervention in protein kinase C (PKC) has a chequered history, partly because of the poor selectivity of many inhibitors and partly a reflection of the sometimes antagonistic action of related PKC isoforms. Recent advances in targeting PKC isoforms have come from structural work on isolated kinase domains that have provided opportunities to drive selectivity through structure-based avenues. The promise of isoform selective inhibitors and the rationale for their development are discussed in the broader context of the PKC inhibitor arsenal.

引用

页码：268 / 279

页数：12

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