Abstract
The deubiquitylating enzyme USP7 (HAUSP) sits at a critical node regulating the activities of numerous proteins broadly characterized as tumor suppressors, DNA repair proteins, immune responders, viral proteins, and epigenetic modulators. Aberrant USP7 activity may promote oncogenesis and viral disease making it a compelling target for therapeutic intervention. Disclosed drug discovery programs have identified inhibitors of USP7 such as P005091 with cellular proof of concept and anti-proliferative activity in cancer models. Taken together, USP7 inhibitors hold promise as a new strategy for the treatment of disease.
Publication types
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Research Support, N.I.H., Extramural
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Review
MeSH terms
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Apoptosis / drug effects
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Colorectal Neoplasms / genetics
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Colorectal Neoplasms / metabolism
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Colorectal Neoplasms / pathology
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Cyclin-Dependent Kinase Inhibitor p21 / metabolism*
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Drug Screening Assays, Antitumor
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HCT116 Cells
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Humans
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Indenes / pharmacology
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Protease Inhibitors / pharmacology*
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Pyrazines / pharmacology
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Tumor Suppressor Protein p53 / metabolism*
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Ubiquitin Thiolesterase / antagonists & inhibitors*
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Ubiquitin Thiolesterase / metabolism
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Ubiquitin-Specific Peptidase 7
Substances
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CDKN1A protein, human
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Cyclin-Dependent Kinase Inhibitor p21
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HBX 41,108
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Indenes
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Protease Inhibitors
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Pyrazines
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Tumor Suppressor Protein p53
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USP7 protein, human
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Ubiquitin Thiolesterase
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Ubiquitin-Specific Peptidase 7