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Updated: Jun 14, 2025

Vasodilation of Isolated Vessels and the Isolation of the Extracellular Matrix of Tight-skin Mice
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NRF2 inhibitors: Recent progress, future design and therapeutic potential

Bingbing Lv1, Shuaishuai Xing2, Zhiqiang Wang1

  • 1School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, People's Republic of China.

European Journal of Medicinal Chemistry
|September 6, 2024
PubMed

Insights

Nuclear factor erythroid 2-related factor 2 (NRF2) inhibitors show promise in overcoming chemotherapy drug resistance. This review comprehensively analyzes the NRF2 pathway, inhibitors, and future development strategies for improved cancer treatment outcomes.

Area of Science:

  • Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • Nuclear factor erythroid 2-related factor 2 (NRF2) is a key regulator of oxidative stress response.
  • Constitutive NRF2 activation is linked to chemotherapy resistance and poor prognosis in cancer patients.

Purpose of the Study:

  • To provide a comprehensive review of NRF2 inhibitors for cancer therapy.
  • To analyze the NRF2 signaling pathway, its regulation, and current inhibitor designs.
  • To discuss future prospects for developing novel NRF2 inhibitors.

Main Methods:

  • Literature review of NRF2 signaling pathway.
  • Systematic search and analysis of reported NRF2 inhibitors.
  • Discussion of structure-activity relationships and design strategies.

Main Results:

  • Detailed overview of NRF2 pathway components and regulation mechanisms.
  • Compilation and categorization of various NRF2 inhibitors.
  • Identification of challenges and opportunities in NRF2 inhibitor development.

Conclusions:

  • NRF2 inhibitors represent a promising strategy to combat drug resistance in cancer.
  • Further research into NRF2 inhibitor design is crucial for clinical translation.
  • This review serves as a foundation for future development of effective NRF2-targeted therapies.
Keywords:
Chemotherapy resistanceNRF2 inhibitorsNRF2-KEAP1 signaling

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