School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, People's Republic of China.
School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, People's Republic of China.
Eur J Med Chem. 2024 Dec 5;279:116822. doi: 10.1016/j.ejmech.2024.116822. Epub 2024 Sep 3.
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.
核因子红细胞 2 相关因子 2（NRF2）是一种参与氧化应激反应的关键转录因子，它控制着各种细胞保护基因的表达。最近的研究表明，持续激活的 NRF2 可以增强患者对化疗药物的耐药性，导致预后不良。因此，开发 NRF2 抑制剂已成为克服癌症治疗中药物耐药性的一种有前途的方法。然而，目前针对 NRF2 抑制剂的报道和综述有限。本综述旨在全面分析 NRF2 信号通路的结构和调节，随后对报道的 NRF2 抑制剂进行全面综述。此外，还将讨论 NRF2 抑制剂的当前设计策略和未来前景，旨在为开发更有效的 NRF2 抑制剂奠定基础。
