Journal
FREE RADICAL BIOLOGY AND MEDICINE
Volume 99, Issue -, Pages 544-556Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.freeradbiomed.2016.09.010
Keywords
Nrf2; ARE; Inhibitor; Chemoresistance; Cancer therapy
Funding
- Chinese Nature Science Foundation [81502841, 81573187, 81573106]
- China Medical University, China
- Liaoning Pandeng Scholar
- National Key Technology Research and Development Program [2014BAI12B02]
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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. (C) 2016 Elsevier Inc. All rights reserved.
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