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    Biochem Soc Trans. 2008 Oct;36(Pt 5):828-32.

    Strategies for the identification of novel inhibitors of deubiquitinating enzymes.

    Goldenberg SJ, McDermott JL, Butt TR, Mattern MR, Nicholson B.

    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; yet toxicity with this target remains high. DUBs (deubiquitinating enzymes) represent an alternative target in the UPS with low predicted toxicity. Currently, there are no DUB inhibitors that have been used clinically. To address this situation, Progenra has developed a novel assay to measure the proteolytic cleavage of Ub (ubiquitin) or UBL (Ub-like protein) conjugates such as SUMO (small Ub-related modifier), NEDD8 (neural-precursor-cell-expressed, developmentally down-regulated 8) or ISG15 (interferon-stimulated gene 15) by isopeptidases. In this review, current platforms for detecting DUB inhibitors are discussed and the advantages and disadvantages of the approaches are underlined.

    PMID:
    18793145
    [PubMed - indexed for MEDLINE]
    PMCID: PMC3061546
    Free PMC Article

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