Advances in deubiquitinating enzyme inhibition and applications in cancer therapeutics

Ainsley Mike Antao, Apoorvi Tyagi, Kye Seong Kim, Suresh Ramakrishna

Research output: Contribution to journalReview article

1 Scopus citations


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.

Original languageEnglish
Article number1579
Pages (from-to)1-36
Number of pages36
Issue number6
StatePublished - 2020 Jun


  • Cancer therapy
  • Deubiquitinase
  • DUB inhibitors
  • Signaling pathways
  • USPs phylogenetic tree

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