The design and development of covalent protein-protein interaction inhibitors for cancer treatment

Sha Sha Cheng, Guan Jun Yang, Wanhe Wang, Chung Hang Leung*, Edmond Dik Lung MA

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

10 Citations (Scopus)

Abstract

Protein-protein interactions (PPIs) are central to a variety of biological processes, and their dysfunction is implicated in the pathogenesis of a range of human diseases, including cancer. Hence, the inhibition of PPIs has attracted significant attention in drug discovery. Covalent inhibitors have been reported to achieve high efficiency through forming covalent bonds with cysteine or other nucleophilic residues in the target protein. Evidence suggests that there is a reduced risk for the development of drug resistance against covalent drugs, which is a major challenge in areas such as oncology and infectious diseases. Recent improvements in structural biology and chemical reactivity have enabled the design and development of potent and selective covalent PPI inhibitors. In this review, we will highlight the design and development of therapeutic agents targeting PPIs for cancer therapy.

Original languageEnglish
Article number26
JournalJournal of Hematology and Oncology
Volume13
Issue number1
DOIs
Publication statusPublished - 30 Mar 2020

Scopus Subject Areas

  • Molecular Biology
  • Hematology
  • Oncology
  • Cancer Research

User-Defined Keywords

  • Cancer therapy
  • Covalent inhibitors
  • Protein-protein interaction

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