Emerging Screening Approaches in the Development of Nrf2–Keap1 Protein–Protein Interaction Inhibitors

Chung Hang Leung, Jia Tong Zhang, Guan Jun Yang, Hao Liu, Simon Q B Han, Edmond Dik Lung Ma*

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

38 Citations (Scopus)


Due to role of the Keap1-Nrf2 protein-protein interaction (PPI) in protecting cells from oxidative stress, the development of small molecule inhibitors that inhibit this interaction has arisen as a viable approach to combat maladies caused by oxidative stress, such as cancers, neurodegenerative disease and diabetes. To obtain specific and genuine Keap1-Nrf2 inhibitors, many efforts have been made towards developing new screening approaches. However, there is no inhibitor for this target entering the clinic for the treatment of human diseases. New strategies to identify novel bioactive compounds from large molecular databases and accelerate the developmental process of the clinical application of Keap1-Nrf2 protein-protein interaction inhibitors are greatly needed. In this review, we have summarized virtual screening and other methods for discovering new lead compounds against the Keap1-Nrf2 protein-protein interaction. We also discuss the advantages and limitations of different strategies, and the potential of this PPI as a drug target in disease therapy.

Original languageEnglish
Article number4445
Number of pages19
JournalInternational Journal of Molecular Sciences
Issue number18
Publication statusPublished - 2 Sept 2019

Scopus Subject Areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

User-Defined Keywords

  • Inhibitors
  • Keap1-Nrf2
  • Oxidative stress
  • Protein-protein interaction
  • Virtual screening


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