An overview of chemical inhibitors of the Nrf2-ARE signaling pathway and their potential applications in cancer therapy

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• 作者：Jiayu Zhu^a ; ¹ ; Huihui Wang^a ; ¹ ; Feng Chen^b ; Jingqi Fu^a ; Yuanyuan Xu^a ; ^{yyxu@cmu.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; Yongyong Hou^a ; Henry H. Kou^a ; Cheng Zhai^a ; M. Bud Nelson^c ; Qiang Zhang^d ; Melvin E. Andersen^e ; Jingbo Pi^a ; ^{jbpi@cmu.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; ^{jingbopi@163.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：AA ; Ascorbic acid ; AEM1 ; ARE expression modulator 1 ; AEG1 ; Astrocyte elevated gene-1 ; Akt ; Protein kinase B ; AMPK ; AMP-activated protein kinase ; APL ; Acute promyelocytic leukemia ; ARE ; Antioxidant response element ; ATO ; Arsenic trioxide ; Bach ; BTB and CNC homology ; Bcl-2 ; B-cell lymphoma-2 ; Bcl-xL ; B-cell lymphoma-extra large ; bRaf ; Proto-oncogene b-Raf ; BTB ; Broad complex ; tramtrack and bric-a-brac ; β-TrCP ; Beta-transducin repeats-containing proteins ; CNC ; Cap &lsquo ; n&rsquo ; Collar ; Cul3 ; Cull
• 刊名：Free Radical Biology and Medicine
• 出版年：2016
• 出版时间：October 2016
• 年：2016
• 卷：99
• 期：Complete
• 页码：544-556
• 全文大小：1306 K

文摘

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.