期刊
FUTURE MEDICINAL CHEMISTRY
卷 12, 期 3, 页码 243-267出版社
FUTURE SCI LTD
DOI: 10.4155/fmc-2019-0285
关键词
chemosensitizer; multidrug resistance; Nrf2 inhibitor
资金
- National Natural Science Foundation of China [81573281, 81872728, 81973207]
- Natural Science Foundation of Jiangsu Province [BK20191411]
- Double First-Classinitiative Innovation team project of China Pharmaceutical University [CPU2018GF11, CPU2018GY34]
- Jiangsu Qinglan Project
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. [GRAPHICS] .
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