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Updated: Apr 29, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists

Published on: November 15, 2013

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Modulation of NRF2 signaling pathway by nuclear receptors: implications for cancer

Akhileshwar Namani1, Yulong Li1, Xiu Jun Wang2

  • 1Department of Biochemistry and Genetics, Zhejiang University School of Medicine, Hangzhou 310058, PR China.

Biochimica Et Biophysica Acta
|May 24, 2014
PubMed

Insights

Nuclear factor-erythroid 2 p45-related factor 2 (NRF2) regulates cellular defense against stress. Its dual role in disease and cancer highlights the therapeutic potential of nuclear receptor-mediated NRF2 inhibition.

Area of Science:

  • Molecular Biology
  • Cellular Biology
  • Oncology

Background:

  • Nuclear factor-erythroid 2 p45-related factor 2 (NRF2) is a transcription factor crucial for cellular defense against oxidative and electrophilic stress.
  • NRF2 activation is explored for treating oxidative stress-related diseases and cancer prevention, but its constitutive activation in tumors promotes cancer cell survival and therapy resistance.

Purpose of the Study:

  • This review provides an overview of the NRF2 signaling pathway and its involvement in carcinogenesis.
  • It introduces the concept of NRF2 inhibition by nuclear receptors and discusses its biological significance in health and disease.
  • The review further explores the potential impact of nuclear receptor-mediated NRF2 inhibition on cancer therapy.

Main Methods:

  • Literature review of NRF2 signaling pathway.
  • Analysis of NRF2's role in carcinogenesis.
  • Examination of nuclear receptor-mediated inhibition of NRF2.
  • Discussion of biological significance and therapeutic implications.

Main Results:

  • NRF2 is a key regulator of antioxidant response genes.
  • Constitutive NRF2 activation contributes to cancer progression and treatment resistance.
  • Nuclear receptors can inhibit NRF2 activity.
  • Regulation of NRF2 by nuclear receptors has implications for both health and disease.

Conclusions:

  • NRF2 plays a complex role in cancer, acting as both a protective factor and a driver of tumor growth.
  • Nuclear receptor-mediated inhibition of NRF2 presents a promising therapeutic strategy for cancer treatment.
  • Further research into this regulatory mechanism could lead to novel anticancer therapies.
Keywords:
Cancer therapyKEAP1NRF2Neh7Nuclear receptor

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