化学
调节器
KEAP1型
小分子
氧化应激
蛋白质-蛋白质相互作用
肽
化学生物学
计算生物学
生物化学
生物
转录因子
基因
作者
Yi Mou,Shuai Wen,Yuxiu Li,Xinxing Gao,Xin Zhang,Zhengyu Jiang
标识
DOI:10.1016/j.ejmech.2020.112532
摘要
Therapeutic targeting the protein-protein interaction (PPI) of Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and its main regulator, Kelch-like ECH-Associating protein 1 (Keap1) has been emerged as a feasible way to combat oxidative stress related diseases, due to the key role of Nrf2 in oxidative stress regulation. In recent years, many efforts have been made to develop potent Keap1-Nrf2 inhibitors with new chemical structures. Various molecules with diverse chemical structures have been reported and some compounds exhibit high potency. This review summarizes peptide and small molecule Keap1-Nrf2 inhibitors reported recently. We also highlight the pharmacological effects and discuss the possible therapeutic application of Keap1-Nrf2 inhibitors.
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