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- W3048771006 abstract "The transcription factor NRF2 (nuclear factor erythroid 2-related factor 2) triggers homeostatic responses against a plethora of environmental or endogenous deviations in redox metabolism, inflammation, proteostasis, etc. Therefore, pharmacological activation of NRF2 is a promising therapeutic strategy for several chronic diseases that are underlined by low-grade oxidative inflammation and dysregulation of redox metabolism, such as neurodegenerative, cardiovascular, and metabolic diseases. While NRF2 activation is useful in inhibiting carcinogenesis, its inhibition is needed in constituted tumors where NRF2 provides a survival advantage in the challenging tumor niche. This review describes the electrophilic and non-electrophilic NRF2 activators with clinical projection in various chronic diseases. We also analyze the status of NRF2 inhibitors, which are for the moment in a proof-of-concept stage. Advanced in silico screening and medicinal chemistry are expected to provide new or repurposing small molecules with increased potential for fostering the development of targeted NRF2 modulators." @default.
- W3048771006 created "2020-08-18" @default.
- W3048771006 creator A5014629533 @default.
- W3048771006 creator A5026807835 @default.
- W3048771006 creator A5067010957 @default.
- W3048771006 creator A5088691369 @default.
- W3048771006 date "2020-01-01" @default.
- W3048771006 modified "2023-09-24" @default.
- W3048771006 title "Perspectives on the Clinical Development of NRF2-Targeting Drugs" @default.
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