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Biochem Soc Trans. 2010 Feb;38(Pt 1):132-6. doi: 10.1042/BST0380132.

Strategies for the identification of ubiquitin ligase inhibitors.

Author information

1
Progenra Inc., 271A Great Valley Parkway, Malvern, PA 19355, USA. goldenberg@progenra.com

Abstract

Dysregulation of the UPS (ubiquitin-proteasome system) has been implicated in a wide range of pathologies including cancer, neurodegeneration and viral infection. Inhibiting the proteasome has been shown to be an effective therapeutic strategy in humans; however, toxicity with this target remains high. E3s (Ub-protein ligases) represent an alternative attractive therapeutic target in the UPS. In this paper, we will discuss current platforms that report on E3 ligase activity and can detect E3 inhibitors, and underline the advantages and disadvantages of each approach.

PMID:
20074047
PMCID:
PMC3060714
DOI:
10.1042/BST0380132
[Indexed for MEDLINE]
Free PMC Article

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