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The Keap1/Nrf2 pathway in health and disease: from the bench to the clinic
Maria A O'Connell1, John D Hayes2
1School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich, NR4 7TJ, U.K. m.oconnell@uea.ac.uk.
Abstract:
The transcription factor nuclear factor-erythroid 2 p45-related factor 2 (Nrf2, with gene called NFE2L2) is a master regulator of the antioxidant response. In the last decade, interest has intensified in this research area as its importance in several physiological and pathological processes has become widely recognized; these include redox signalling and redox homoeostasis, drug metabolism and disposition, intermediary metabolism, cellular adaptation to stress, chemoprevention and chemoresistance, toxicity, inflammation, neurodegeneration, lipogenesis and aging. Regulation of Nrf2 is complex and although much attention has focussed on its repression by Kelch-like ECH-associated protein-1 (Keap1), recently it has become increasingly apparent that it is also controlled by cross-talk with other signalling pathways including the glycogen synthase kinase-3 (GSK-3)-β-transducin repeat-containing protein (β-TrCP) axis, ERAD (endoplasmic reticulum-associated degradation)-associated E3 ubiquitin-protein ligase (Hrd1, also called synoviolin), nuclear factor-kappa B (NF-κB), Notch and AMP kinase. Due to its beneficial role in several diseases, Nrf2 has become a major therapeutic target, with novel natural, synthetic and targeted small molecules currently under investigation to modulate the pathway and in clinical trials.
Insights
Nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) is a key regulator of cellular antioxidant responses. Its complex regulation and therapeutic potential in various diseases are increasingly recognized, making it a significant drug target.
Area of Science:
- Molecular Biology
- Cellular Biology
- Biochemistry
Background:
- Nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) is a master regulator of the antioxidant response.
- Its role in physiological and pathological processes like redox signaling, metabolism, and aging is widely acknowledged.
- Nrf2 is implicated in cellular adaptation to stress, drug metabolism, inflammation, and neurodegeneration.
Purpose of the Study:
- To highlight the complex regulatory mechanisms of Nrf2.
- To underscore the growing therapeutic interest in Nrf2 modulation for various diseases.
- To review the cross-talk of Nrf2 with other signaling pathways.
Main Methods:
- Literature review focusing on Nrf2 regulation and function.
- Analysis of Nrf2's interaction with key signaling pathways like Keap1, GSK-3/β-TrCP, and NF-κB.
- Examination of Nrf2's role in disease pathogenesis and therapeutic strategies.
Main Results:
- Nrf2 regulation involves intricate cross-talk with multiple signaling pathways beyond Keap1.
- Pathways such as GSK-3/β-TrCP, Hrd1, NF-κB, Notch, and AMP kinase influence Nrf2 activity.
- Nrf2's involvement spans diverse processes including chemoprevention, chemoresistance, toxicity, and aging.
Conclusions:
- Nrf2 is a crucial target for therapeutic intervention due to its beneficial roles in disease.
- Modulating the Nrf2 pathway holds promise for treating conditions related to oxidative stress and inflammation.
- Ongoing research focuses on developing novel small molecules to target the Nrf2 pathway in clinical trials.
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