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

作者：Zhu Jiayu; Wang Huihui; Chen Feng; Fu Jingqi; Xu Yuanyuan; Hou Yongyong; Kou Henry H; Zhai Cheng; Nelson Bud; Zhang Qiang; Andersen Melvin E; Pi Jingbo

来源：Free Radical Biology and Medicine, 2016, 99: 544-556.

DOI：10.1016/j.freeradbiomed.2016.09.010

• Nrf2
• ARE
• Inhibitor
• Chemoresistance
• Cancer therapy

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.

• 出版日期2016-10
• 单位中国医科大学