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.
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October 2008
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Conference Article|
September 19 2008
Strategies for the identification of novel inhibitors of deubiquitinating enzymes
Seth J. Goldenberg;
Seth J. Goldenberg
1
1Progenra Inc., 271A Great Valley Parkway, Malvern, PA 19355, U.S.A.
1To whom correspondence should be addressed (email [email protected]).
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Jeffrey L. McDermott;
Jeffrey L. McDermott
1Progenra Inc., 271A Great Valley Parkway, Malvern, PA 19355, U.S.A.
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Tauseef R. Butt;
Tauseef R. Butt
1Progenra Inc., 271A Great Valley Parkway, Malvern, PA 19355, U.S.A.
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Michael R. Mattern;
Michael R. Mattern
1Progenra Inc., 271A Great Valley Parkway, Malvern, PA 19355, U.S.A.
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Benjamin Nicholson
Benjamin Nicholson
1Progenra Inc., 271A Great Valley Parkway, Malvern, PA 19355, U.S.A.
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Publisher: Portland Press Ltd
Received:
March 03 2008
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© The Authors Journal compilation © 2008 Biochemical Society
2008
Biochem Soc Trans (2008) 36 (5): 828–832.
Article history
Received:
March 03 2008
Citation
Seth J. Goldenberg, Jeffrey L. McDermott, Tauseef R. Butt, Michael R. Mattern, Benjamin Nicholson; Strategies for the identification of novel inhibitors of deubiquitinating enzymes. Biochem Soc Trans 1 October 2008; 36 (5): 828–832. doi: https://doi.org/10.1042/BST0360828
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