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Activators and Inhibitors of NRF2: A Review of Their Potential for Clinical Development

Robledinos-Antón, Natalia, Fernández-Ginés, Raquel, Manda, Gina, Cuadrado, Antonio·2019·Oxidative Medicine and Cellular Longevity
DOI 10.1155/2019/9372182PMC PMC6664516
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Abstract

The transcription factor NRF2 (nuclear factor erythroid 2-related factor 2) triggers the first line of homeostatic responses against a plethora of environmental or endogenous deviations in redox metabolism, proteostasis, inflammation, etc. Therefore, pharmacological activation of NRF2 is a promising therapeutic approach for several chronic diseases that are underlined by oxidative stress and inflammation, such as neurodegenerative, cardiovascular, and metabolic diseases. A particular case is cancer, where NRF2 confers a survival advantage to constituted tumors, and therefore, NRF2 inhibition is desired. This review describes the electrophilic and nonelectrophilic NRF2 activators with clinical projection in various chronic diseases. We also analyze the status of NRF2 inhibitors, which at this time provide proof of concept for blocking NRF2 activity in cancer therapy.

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Metadata

Authors
Robledinos-Antón, N., Fernández-Ginés, R., Manda, G., & Cuadrado, A.
Affiliations
  • Instituto de Investigaciones Biomédicas “Alberto Sols” UAM-CSIC, Instituto de Investigación Sanitaria La Paz (IdiPaz) and Department of Biochemistry, Faculty of Medicine, Autonomous University of Madrid, Madrid, Spain
  • Victor Babes National Institute of Pathology, Bucharest, Romania
ORCID
Venue
Oxidative Medicine and Cellular Longevity
Publisher
Wiley
Published
2019-07-14
Volume
2019
Pages
1-20
ISSN
  • 1942-0900
  • 1942-0994
DOI
10.1155/2019/9372182
PMC
PMC6664516
Cited by
413
References
16
Language
en
Licence
creativecommons.org/licenses/by/4.0/ (unspecified)
Funders
  • European Regional Development Fund (P_37_732/2016, B2017/BMD-3827, SAF2016-76520-R)
  • Autonomous Community of Madrid (P_37_732/2016, B2017/BMD-3827, SAF2016-76520-R)
  • Ministerio de Economía y Competitividad (P_37_732/2016, B2017/BMD-3827, SAF2016-76520-R)

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