Therapeutic strategies within the ubiquitin proteasome system

被引：104

作者：

Eldridge, A. G. ^{[1
]}

O'Brien, T. ^{[1
]}

机构：

[1] Genentech Inc, Dept Cell Regulat, San Francisco, CA 94080 USA

来源：

CELL DEATH AND DIFFERENTIATION | 2010年 / 17卷 / 01期

关键词：

ubiquitin; E3; ligase; DUB; proteasome; small molecule inhibitor; CONJUGATING ENZYME; LIGASE ACTIVITY; RING FINGER; IN-VITRO; STRUCTURAL INSIGHTS; P53; PATHWAY; U-BOX; PROTEIN; ACTIVATION; INHIBITORS;

D O I：

10.1038/cdd.2009.82

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：

The ubiquitin-dependent proteolysis system (UPS) is the main driver of regulated protein degradation in all eukaryotic cells, and it is becoming increasingly clear that defects within this pathway drive a large number of human pathologies. Recent success in the use of proteasome inhibitors in the treatment of hematological malignancies validates the UPS as a viable therapeutic pathway, and substantial effort is now focused on the development of both second-generation proteasome inhibitors as well as novel strategies for the inhibition of upstream UPS enzymes. In this review we discuss the potential 'druggability' of key nodes within the UPS and summarize recent advances within the field. Cell Death and Differentiation (2010) 17, 4-13; doi:10.1038/cdd.2009.82; published online 26 June 2009

引用

页码：4 / 13

页数：10

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