Related Experiment Video

Updated: Feb 19, 2026

Protocol for the Differentiation of Human Induced Pluripotent Stem Cells into Mixed Cultures of Neurons and Glia for Neurotoxicity Testing
09:02

Protocol for the Differentiation of Human Induced Pluripotent Stem Cells into Mixed Cultures of Neurons and Glia for Neurotoxicity Testing

Published on: June 9, 2017

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NRF2-targeted therapeutics: New targets and modes of NRF2 regulation

Montserrat Rojo de la Vega1, Matthew Dodson1, Eli Chapman1

  • 1Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, AZ, USA, 85721.

Current Opinion in Toxicology
|October 31, 2017
PubMed

Insights

Targeting the NRF2 pathway offers therapeutic potential for chronic diseases. However, understanding NRF2

Area of Science:

  • Molecular Biology
  • Cellular Biology
  • Pharmacology

Background:

  • Nuclear factor-erythroid derived 2-like 2 (NRF2) regulates cellular antioxidant responses.
  • NRF2 activation shows potential in preventing oxidative stress, carcinogenesis, diabetes, and chronic kidney disease.
  • The "dark side" of NRF2 involves tissue damage, cancer progression, and chemoresistance with prolonged activation.

Purpose of the Study:

  • To review available and potential NRF2-targeted therapeutics.
  • To discuss the mechanisms of action for NRF2-targeted drugs.
  • To explore the potential of NRF2 therapeutics in disease prevention and treatment.

Main Methods:

  • Review of current literature on NRF2 activators and inhibitors.
  • Analysis of NRF2 regulatory mechanisms, including KEAP1-dependent and independent pathways.
  • Discussion of therapeutic strategies targeting NRF2.

Main Results:

  • One NRF2 activator is clinically approved; no specific inhibitors are currently discovered.
  • Emerging understanding of NRF2 degradation pathways offers new therapeutic avenues.
  • NRF2-targeted therapeutics present diverse modes of action for disease management.

Conclusions:

  • NRF2-targeted therapies hold promise for various chronic conditions.
  • Further research into NRF2 regulation is crucial for developing safe and specific therapeutics.
  • Balancing NRF2 activation and inhibition is key for effective therapeutic strategies.
Keywords:
NRF2autophagycancerchemopreventiondiabeteselectrophiles

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