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Nat Rev Drug Discov. 2018 Jan;17(1):57-78. doi: 10.1038/nrd.2017.152. Epub 2017 Sep 29.

Deubiquitylating enzymes and drug discovery: emerging opportunities.

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Mission Therapeutics Ltd, Moneta, Babraham Research Campus, Cambridge CB22 3AT, UK.
Artios Pharmaceuticals Ltd, Maia, Babraham Research Campus, Cambridge CB22 3AT, UK.
The Wellcome Trust and Cancer Research UK Gurdon Institute, and Department of Biochemistry, Tennis Court Road, University of Cambridge, Cambridge CB2 1QN, UK.


More than a decade after a Nobel Prize was awarded for the discovery of the ubiquitin-proteasome system and clinical approval of proteasome and ubiquitin E3 ligase inhibitors, first-generation deubiquitylating enzyme (DUB) inhibitors are now approaching clinical trials. However, although our knowledge of the physiological and pathophysiological roles of DUBs has evolved tremendously, the clinical development of selective DUB inhibitors has been challenging. In this Review, we discuss these issues and highlight recent advances in our understanding of DUB enzymology and biology as well as technological improvements that have contributed to the current interest in DUBs as therapeutic targets in diseases ranging from oncology to neurodegeneration.

[Indexed for MEDLINE]

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