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Advances in Deubiquitinating Enzyme Inhibition and Applications in Cancer Therapeutics

Graduate School of Biomedical Science and Engineering, Hanyang University, Seoul 04763, Korea
College of Medicine, Hanyang University, Seoul 04763, Korea
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Cancers 2020, 12(6), 1579;
Received: 24 April 2020 / Revised: 7 June 2020 / Accepted: 11 June 2020 / Published: 15 June 2020
(This article belongs to the Special Issue Targeting the Ubiquitin Pathway in Cancer)
Since the discovery of the ubiquitin proteasome system (UPS), the roles of ubiquitinating and deubiquitinating enzymes (DUBs) have been widely elucidated. The ubiquitination of proteins regulates many aspects of cellular functions such as protein degradation and localization, and also modifies protein-protein interactions. DUBs cleave the attached ubiquitin moieties from substrates and thereby reverse the process of ubiquitination. The dysregulation of these two paramount pathways has been implicated in numerous diseases, including cancer. Attempts are being made to identify inhibitors of ubiquitin E3 ligases and DUBs that potentially have clinical implications in cancer, making them an important target in the pharmaceutical industry. Therefore, studies in medicine are currently focused on the pharmacological disruption of DUB activity as a rationale to specifically target cancer-causing protein aberrations. Here, we briefly discuss the pathophysiological and physiological roles of DUBs in key cancer-related pathways. We also discuss the clinical applications of promising DUB inhibitors that may contribute to the development of DUBs as key therapeutic targets in the future. View Full-Text
Keywords: cancer therapy; deubiquitinase; DUB inhibitors; USPs phylogenetic tree; signaling pathways cancer therapy; deubiquitinase; DUB inhibitors; USPs phylogenetic tree; signaling pathways
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MDPI and ACS Style

Antao, A.M.; Tyagi, A.; Kim, K.-S.; Ramakrishna, S. Advances in Deubiquitinating Enzyme Inhibition and Applications in Cancer Therapeutics. Cancers 2020, 12, 1579.

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