Abstract
The basic leucine zipper transcription factor Nrf2 is the primary regulator of cellular oxidative stress. Activation of Nrf2 is regarded as a potential preventive and therapeutic strategy. However, aberrant hyperactivation of Nrf2 is found in a variety of cancers and promotes cancer progression and metastasis. Moreover, constitutive activation of Nrf2 confers cancer cells resistance to chemo- and radio-therapy. Thus, inhibiting Nrf2 could be a new therapeutic strategy for cancer. With the aim of accelerating the discovery and development of novel Nrf2 inhibitors, we summarize the biological and pathological functions of Nrf2 in cancer. Furthermore, the recent studies of small molecular Nrf2 inhibitors and potential Nrf2 inhibitory mechanisms are also summarized in this review.
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Financial & competing interests disclosure
The authors gratefully thank the support from the grants (nos. 81573281, 81872728 and 81973207) of National Natural Science Foundation of China, (nos. BK20191411) of Natural Science Foundation of Jiangsu Province. The authors thank the support from Double First-Class” initiative Innovation team project of China Pharmaceutical University (nos. CPU2018GF11 and CPU2018GY34), and Jiangsu Qinglan Project (Yao Chen). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.
No writing assistance was utilized in the production of this manuscript.