Frontiers in Pharmacology (Apr 2019)

USP7: Novel Drug Target in Cancer Therapy

  • Zhiru Wang,
  • Zhiru Wang,
  • Zhiru Wang,
  • Wenting Kang,
  • Wenting Kang,
  • Yinghua You,
  • Yinghua You,
  • Jingru Pang,
  • Jingru Pang,
  • Hongmei Ren,
  • Hongmei Ren,
  • Zhenhe Suo,
  • Hongmin Liu,
  • Hongmin Liu,
  • Yichao Zheng,
  • Yichao Zheng

DOI
https://doi.org/10.3389/fphar.2019.00427
Journal volume & issue
Vol. 10

Abstract

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Ubiquitin specific protease 7 (USP7) is one of the deubiquitinating enzymes (DUB) that erases ubiquitin and protects substrate protein from degradation. Full activity of USP7 requires the C-terminal Ub-like domains fold back onto the catalytic domain, allowing the remodeling of the active site to a catalytically competent state by the C-terminal peptide. Until now, numerous proteins have been identified as substrates of USP7, which play a key role in cell cycle, DNA repair, chromatin remodeling, and epigenetic regulation. Aberrant activation or overexpression of USP7 may promote oncogenesis and viral disease, making it a target for therapeutic intervention. Currently, several synthetic small molecules have been identified as inhibitors of USP7, and applied in the treatment of diverse diseases. Hence, USP7 may be a promising therapeutic target for the treatment of cancer.

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