2. Academic Validation
  3. NRF2 inhibitors: Recent progress, future design and therapeutic potential

NRF2 inhibitors: Recent progress, future design and therapeutic potential

  • Eur J Med Chem. 2024 Dec 5:279:116822. 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 4,  Yao Chen 5
Affiliations

Affiliations

  • 1 School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, People's Republic of China.
  • 2 School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, People's Republic of China.
  • 3 Jiangsu Provincial Engineering Center of TCM External Medication Researching and Industrializing, Nanjing University of Chinese Medicine, Nanjing, 210023, People's Republic of China.
  • 4 School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, People's Republic of China. Electronic address: [email protected].
  • 5 School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, People's Republic of China. Electronic address: [email protected].
PMID: 39241669 DOI: 10.1016/j.ejmech.2024.116822
Abstract

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.

Keywords

Chemotherapy resistance; NRF2 inhibitors; NRF2-KEAP1 signaling.

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