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PMID: 20074047 Published · ppublish English Journal Article Research Support, N.I.H., Extramural Review

Strategies for the identification of ubiquitin ligase inhibitors.

Biochemical Society transactions ·Vol. 38 ·No. Pt 1 ·2010-02-00 ·Pages 132-6

Goldenberg SJ, Marblestone JG, Mattern MR, Nicholson B

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.

MeSH Terms
Biological Assay/methods Humans Immune System Diseases/drug therapy,enzymology Neoplasms/drug therapy,enzymology Neurodegenerative Diseases/drug therapy,enzymology Protease Inhibitors/metabolism Proteasome Endopeptidase Complex/metabolism Proteasome Inhibitors Ubiquitin/metabolism Ubiquitin-Protein Ligases/antagonists & inhibitors,metabolism
Chemicals
Protease Inhibitors Proteasome Inhibitors Ubiquitin Ubiquitin-Protein Ligases Proteasome Endopeptidase Complex
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Goldenberg Seth J
Progenra Inc., 271A Great Valley Parkway, Malvern, PA 19355, USA. goldenberg@progenra.com
Marblestone Jeffrey G
Mattern Michael R
Nicholson Benjamin
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Article Info
Journal
Biochemical Society transactions
Abbr.
Biochem Soc Trans
ISSN
1470-8752
DOI
10.1042/BST0380132
Email
goldenberg@progenra.com
Published
2010-02-00
Pages
132-6
Language
English
Region
England
NLM ID
7506897
PMCID
PMC3060714
Subset
IM
Grants
NCI NIH HHS · R43 CA119605-01 · United States
NIA NIH HHS · AG025568 · United States
NIA NIH HHS · AG025726 · United States
External Links
PubMed source DOI: 10.1042/BST0380132 PMC Full Text View journal details
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