NRF2 inhibitors: Recent progress, future design and therapeutic potential,European Journal of Medicinal Chemistry

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NRF2 inhibitors: Recent progress, future design and therapeutic potential
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2024-09-03 , DOI: 10.1016/j.ejmech.2024.116822
Bingbing Lv ₁ , Shuaishuai Xing ₂ , Zhiqiang Wang ₁ , Ao Zhang ₁ , Qinjie Wang ₁ , Yaoyao Bian ₃ , Yuqiong Pei ₁ , Haopeng Sun ₂ , Yao Chen ₁

Affiliation

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.

中文翻译：

NRF2 抑制剂的最新进展、未来设计和治疗潜力

核因子红细胞 2 相关因子 2 （NRF2）是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，组成型激活的 NRF2 会增强患者对化疗药物的耐药性，从而导致不良预后。因此，NRF2 抑制剂的开发已成为克服癌症治疗中耐药性的一种有前途的方法。然而，针对 NRF2 抑制剂的报告和评论有限。本综述旨在对 NRF2 信号通路的结构和调节进行全面分析，然后对已报道的 NRF2 抑制剂进行全面综述。此外，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。

更新日期：2024-09-03

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