An overview of chemical inhibitors of the Nrf2-ARE signaling pathway and their potential applications in cancer therapy
Abstract
The Nuclear factor erythroid 2-related factor 2 (Nrf2) is a key transcription factor regulating a wide array of genes for antioxidant and detoxification enzymes in response to oxidative and xenobiotic stress. A large number of Nrf2-antioxidant response element (ARE) activators have been screened for use as chemopreventive agents in oxidative stress-related diseases and even cancer. However, constitutive activation of Nrf2 occurs in a variety of cancers. Aberrant activation of Nrf2 is correlated with cancer progression, chemoresistance, and radioresistance. In this review, we examine recent studies of Nrf2-ARE inhibitors in the context of cancer therapy. We enumerate the possible Nrf2-inhibiting mechanisms of these compounds, their effects sensitizing cancer cells to chemotherapeutic agents, and the prospect of applying them in clinical cancer therapy.
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Research has explored the use of Nrf2 inhibitors as adjuvants to cancer therapy.
“Research has thus also explored the use of Nrf2 inhibitors as adjuvants to cancer therapy [226,228].”
From Nrf2 and Oxidative Stress: A General Overview of Mechanisms and Implications in Human Disease (2022) · cites this paper as [228]
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References 205 · Cited by 162
- Authors
- Zhu, J., Wang, H., Chen, F., Fu, J., Xu, Y., Hou, Y., Kou, H. H., Zhai, C., Nelson, M. B., Zhang, Q., Andersen, M. E., & Pi, J.
- Affiliations
- China Medical University (CN)
- First Hospital of China Medical University (CN)
- Emory University (US)
- The Hamner Institutes for Health Sciences (US)
- Corresponding author
- Xu, Yuanyuan
- Pi, Jingbo
- ORCID
- Venue
- Free Radical Biology and Medicine
- Publisher
- Elsevier BV
- Published
- 2016-10
- Volume
- 99
- Pages
- 544-556
- ISSN
- 0891-5849 (ISSN-L)
- OpenAlex
- W2520805712
- Cited by
- 162
- References
- 205
- Citations by year
- 2026: 6 · 2025: 7 · 2024: 9 · 2023: 17 · 2022: 15 · 2021: 22 · 2020: 16 · 2019: 21 · 2018: 23 · 2017: 25 · 2016: 1
- FWCI
- 2.11
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Free Radical Biology and Medicine (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Chinese Nature Science Foundation (81502841, 81573187, 81573106)
- China Medical University, China
- Liaoning Pandeng Scholar
- National Key Technology Research and Development Program (2014BAI12B02)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Genomics, phytochemicals, and oxidative stress
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Toxicology › Bioactive Compounds and Antitumor Agents
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Redox biology and oxidative stress
- Keywords
- Nrf2, antioxidant response element, Nrf2 inhibitors, chemoprevention, cancer therapy, oxidative stress, chemoresistance, radioresistance (biology), chemosensitization, antioxidant enzymes, detoxification enzymes, transcription factor regulation
- MeSH terms
- Kelch-Like ECH-Associated Protein 1, Animals, Antineoplastic Agents, Antitubercular Agents, Flavonoids, Humans, Hypoglycemic Agents, Neoplasms, Vitamins, Signal Transduction, Gene Expression Regulation, Neoplastic, Oxidative Stress, Drug Resistance, Neoplasm, Cullin Proteins, NF-E2-Related Factor 2, Antioxidant Response Elements
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