Abstract：
UNASSIGNED: The nuclear factor erythroid 2-related factor 2 (Nrf2) is a pivotal transcription factor that controls the expression of numerous cytoprotective genes and regulates cellular defense system against oxidative insults. Thus, activating the Nrf2 pathway is a promising strategy for the treatment of various chronic diseases characterized by oxidative stress.
UNASSIGNED: This review first discusses the biological effects of Nrf2 and the regulatory mechanism of Kelch-like ECH-associated protein 1-Nrf2-antioxidant response element (Keap1-Nrf2-ARE) pathway. Then, Nrf2 activators (2020-present) are summarized based on the mechanism of action. The case studies consist of chemical structures, biological activities, structural optimization, and clinical development.
UNASSIGNED: Extensive efforts have been devoted to developing novel Nrf2 activators with improved potency and drug-like properties. These Nrf2 activators have exhibited beneficial effects in in vitro and in vivo models of oxidative stress-related chronic diseases. However, some specific problems, such as target selectivity and brain blood barrier (BBB) permeability, still need to be addressed in the future.
UNASSIGNED: This review first discusses the biological effects of Nrf2 and the regulatory mechanism of Kelch-like ECH-associated protein 1-Nrf2-antioxidant response element (Keap1-Nrf2-ARE) pathway. Then, Nrf2 activators (2020-present) are summarized based on the mechanism of action. The case studies consist of chemical structures, biological activities, structural optimization, and clinical development.
UNASSIGNED: Extensive efforts have been devoted to developing novel Nrf2 activators with improved potency and drug-like properties. These Nrf2 activators have exhibited beneficial effects in in vitro and in vivo models of oxidative stress-related chronic diseases. However, some specific problems, such as target selectivity and brain blood barrier (BBB) permeability, still need to be addressed in the future.
摘要：
未经证实：核因子类红细胞2相关因子2（Nrf2）是一种关键的转录因子，可控制许多细胞保护基因的表达并调节细胞防御系统抵抗氧化损伤。因此，激活Nrf2途径是治疗以氧化应激为特征的各种慢性疾病的有希望的策略。
UNASSIGNED:这篇综述首先讨论了Nrf2的生物学效应以及Kelch样ECH相关蛋白1-Nrf2-抗氧化反应元件(Keap1-Nrf2-ARE)通路的调控机制。然后，根据作用机理总结了Nrf2活化剂（2020年至今）。案例研究包括化学结构，生物活动，结构优化,和临床发展。
UNASSIGNED：人们一直在努力开发具有改进效力和类似药物特性的新型Nrf2活化剂。这些Nrf2激活剂在氧化应激相关慢性疾病的体外和体内模型中表现出有益效果。然而,一些具体的问题，如目标选择性和脑血屏障(BBB)通透性，未来仍需解决。
UNASSIGNED:这篇综述首先讨论了Nrf2的生物学效应以及Kelch样ECH相关蛋白1-Nrf2-抗氧化反应元件(Keap1-Nrf2-ARE)通路的调控机制。
UNASSIGNED：人们一直在努力开发具有改进效力和类似药物特性的新型Nrf2活化剂。
