title: Inhibiting the deubiquitinating enzymes (DUBs).
abstract: The diverse roles of deubiquitinating enzymes, or DUBs, in determining the fate of specific proteins continue to unfold. Concurrent with the revelation of DUBs as potential therapeutic targets are publications of small molecule inhibitors of these enzymes. In this review, we summarize these molecules and their associated data and suggest additional experiments to further validate and characterize these compounds. We believe the field of drug discovery against DUBs is still in its infancy, but advances in assay development, biophysical techniques, and screening libraries hold promise for identifying suitable agents that could advance into the clinic.
authors.affiliation: Department of Discovery Chemistry, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
authors.forename: Chudi
authors.initials: C
authors.lastname: Ndubaku
authors.forename: Vickie
authors.initials: V
authors.lastname: Tsui
mesh_terms: D018360:Crystallography, X-Ray; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D064570:Ubiquitin-Specific Proteases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D064570:Ubiquitin-Specific Proteases