TherapeuticsCancer Drug Resistance

NRF2 inhibitors: Recent progress, future design and therapeutic potential

European Journal of Medicinal Chemistry

Abstract

This review comprehensively covers recent progress in NRF2 inhibitor development for overcoming drug resistance in cancer. Details design principles, pharmacological properties, and therapeutic potential of various candidates.

Key Findings

  • Comprehensive catalogue of NRF2 inhibitors under development
  • NRF2 inhibitors classified by mechanism: direct binding, transcriptional suppression, degradation
  • Natural compounds (brusatol, trigonelline) and synthetic molecules under investigation
  • NRF2 inhibitors show synergy with conventional chemotherapy

Clinical Significance

Essential reference for NRF2 drug development pipeline. Provides medicinal chemistry foundation for clinically viable NRF2-targeted therapies.

Citation

NRF2 inhibitors: Progress and potential. (2024). European Journal of Medicinal Chemistry.

DOI: 10.1016/j.ejmech.2024.106845