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

    Strategies for the identification of ubiquitin ligase inhibitors.

    Source

    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
    [PubMed - indexed for MEDLINE]
    PMCID: PMC3060714
    Free PMC Article

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