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.

针对核因子（类胡萝卜素2）样2（Nrf2）及其主要调控因子，Kelch-样ECH-Associating protein 1（Keap1）的蛋白质-蛋白质相互作用（PPI）的治疗方法已成为一种可行的治疗方法Nrf2在氧化应激调节中的关键作用，是与氧化应激相关的疾病。近年来，为开发具有新化学结构的强效Keap1-Nrf2抑制剂做出了许多努力。已经报道了具有不同化学结构的各种分子，并且某些化合物显示出高效力。这篇综述总结了最近报道的肽和小分子Keap1-Nrf2抑制剂。我们还将重点介绍其药理作用，并讨论Keap1-Nrf2抑制剂的可能治疗应用。