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Advances and challenges in therapeutic targeting of NRF2

Albena T Dinkova-Kostova1, Ian M Copple2

  • 1Division of Cellular and Systems Medicine, School of Medicine, University of Dundee, Dundee, DD1 9SY, UK; Department of Pharmacology and Molecular Sciences and Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, MD, USA.

Trends in Pharmacological Sciences
|January 11, 2023
PubMed

Insights

Activating the nuclear factor erythroid 2-related factor 2 (NRF2) pathway combats oxidative stress and inflammation, offering therapeutic potential for chronic diseases. Understanding NRF2 pharmacology is crucial as drug development advances toward clinical applications.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Nuclear factor erythroid 2-related factor 2 (NRF2) activation is a promising therapeutic strategy.
  • Oxidative stress, inflammation, and metabolic imbalances are implicated in chronic diseases like neurodegenerative and metabolic disorders.
  • The NRF2 field is progressing towards clinical applications, necessitating a deeper understanding of its pharmacology.

Purpose of the Study:

  • To outline the rationale for targeting NRF2 therapeutically.
  • To summarize recent advancements in the development of NRF2 modulators.
  • To discuss challenges and future directions for NRF2-based therapies.

Main Methods:

  • Literature review of NRF2 research.
  • Analysis of current drug development pipelines for NRF2 modulators.
  • Discussion of pharmacological principles relevant to NRF2 targeting.

Main Results:

  • NRF2 activation effectively counteracts key pathological processes.
  • Several NRF2-modulating drugs are in various stages of development.
  • Significant challenges remain in optimizing NRF2 pharmacology for clinical success.

Conclusions:

  • Targeting NRF2 holds considerable therapeutic promise for a range of chronic diseases.
  • Continued research into NRF2 pharmacology is essential to overcome developmental hurdles.
  • Realizing the full clinical potential of NRF2 requires addressing current challenges in drug development and application.
Keywords:
KEAP1NRF2chronic diseaseelectrophileinflammationoxidative stress

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