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Recent advances in the development of ubiquitin-specific-processing protease 7 (USP7) inhibitors

Peng Li1, Hong-Min Liu1

  • 1Key Laboratory of Advanced Technology of Drug Preparation Technologies, Ministry of Education, Co-innovation Center of Henan Province for New Drug R & D and Preclinical Safety, And School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.

European Journal of Medicinal Chemistry
|February 25, 2020
PubMed

Insights

This review details small molecule inhibitors targeting Ubiquitin-Specific-Processing Protease 7 (USP7), a key enzyme in cancer research. It covers structures, activities, and development strategies for these promising cancer therapeutics.

Area of Science:

  • Biochemistry
  • Oncology
  • Medicinal Chemistry

Background:

  • Ubiquitin-Specific-Processing Protease 7 (USP7) is a deubiquitinating enzyme implicated in cancer progression.
  • While USP7's role in cancer is recognized, research on its small molecule inhibitors remains limited.
  • Existing reviews often focus on USP7's physiological functions rather than inhibitor development.

Purpose of the Study:

  • To systematically review small molecule USP7 inhibitors disclosed between 2000 and 2019.
  • To summarize their structures, activities, and structure-activity relationships (SAR).
  • To discuss binding modes, interactions, and challenges in developing USP7 inhibitors.

Main Methods:

  • Literature and patent search for small molecule USP7 inhibitors from 2000-2019.
  • Systematic summarization of structural and activity data.
  • Analysis of binding modes and SAR.

Main Results:

  • Compilation of diverse small molecule USP7 inhibitors with detailed SAR.
  • Presentation of typical compound binding modes and USP7 interactions.
  • Overview of other deubiquitinase inhibitors.

Conclusions:

  • Small molecule USP7 inhibitors represent a promising area for cancer therapy development.
  • Understanding SAR and binding modes is crucial for rational drug design.
  • Further strategies are needed to overcome challenges in developing effective USP7 inhibitors.
Keywords:
CancerInhibitorsSARUSP7Ubiquitination

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