NRF2 inhibitors: Recent progress, future design and therapeutic potential

被引:6
作者
Lv, Bingbing [1 ]
Xing, Shuaishuai [2 ]
Wang, Zhiqiang [1 ]
Zhang, Ao [1 ]
Wang, Qinjie [1 ]
Bian, Yaoyao [3 ]
Pei, Yuqiong [1 ]
Sun, Haopeng [2 ]
Chen, Yao [1 ]
机构
[1] Nanjing Univ Chinese Med, Sch Pharm, Nanjing 210023, Peoples R China
[2] China Pharmaceut Univ, Sch Pharm, Nanjing 211198, Peoples R China
[3] Nanjing Univ Chinese Med, Jiangsu Prov Engn Ctr TCM External Medicat Researc, Nanjing 210023, Peoples R China
基金
中国国家自然科学基金;
关键词
NRF2-KEAP1; signaling; NRF2; inhibitors; Chemotherapy resistance; TRANSCRIPTION FACTOR NRF2; LUNG-CANCER CELLS; TYROSINE KINASE INHIBITOR; SMALL-MOLECULE INHIBITORS; ANTIOXIDANT RESPONSE; HEPATOCELLULAR-CARCINOMA; SIGNALING PATHWAY; OXIDATIVE STRESS; GENE-EXPRESSION; IN-VITRO;
D O I
10.1016/j.ejmech.2024.116822
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Nuclear factor erythroid 2-related factor 2 (NRF2) is a crucial transcription factor involved in oxidative stress response, which controls the expression of various cytoprotective genes. Recent research has indicated that constitutively activated NRF2 can enhance patients' resistance to chemotherapy drugs, resulting in unfavorable prognosis. Therefore, the development of NRF2 inhibitors has emerged as a promising approach for overcoming drug resistance in cancer treatment. However, there are limited reports and reviews focusing on NRF2 inhibitors. This review aims to provide a comprehensive analysis of the structure and regulation of the NRF2 signaling pathway, followed by a comprehensive review of reported NRF2 inhibitors. Moreover, the current design strategies and future prospects of NRF2 inhibitors will be discussed, aiming to establish a foundation for the development of more effective NRF2 inhibitors.
引用
收藏
页数:19
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