Strategies for the Identification of Ubiquitin Ligase Inhibitors

Overview

Journal Biochem Soc Trans

Specialty Biochemistry

Date 2010 Jan 16

PMID 20074047

Citations 16

Authors

Seth J Goldenberg

Jeffrey G Marblestone

Michael R Mattern

Benjamin Nicholson

Affiliations

Soon will be listed here.

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.

Citing Articles

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Lizama B, Palubinsky A, McLaughlin B Neurochem Int. 2017; 117:139-155.

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