[关键词]
[摘要]
Nrf2/ARE信号通路是细胞氧化应激反应中的关键通路,其调控的下游抗氧化蛋白和Ⅱ相解毒酶在细胞防御保护中发挥重要作用。现有研究显示Nrf2/ARE通路在抗炎、抗肿瘤、神经保护、抗凋亡等多方面具有重要作用,以Nrf2为靶点的药物有望用于多发性硬化、糖尿病、神经退行性疾病、肿瘤等多种疾病的治疗,其中已有富马酸二甲酯、巴多克沙龙等多个新药进入临床研究阶段。就Nrf2/ARE通路与疾病的关系及以其为靶点的新药研发进展做一综述。
[Key word]
[Abstract]
Nrf2/antioxidant-response-element (ARE) signal pathway is vital in the regulation of cellular oxidative stress response, and the downstream anti-oxidant proteins and phase Ⅱ detoxification enzyme, which were regulated by Nrf2/ARE pathway, play the important roles in the cellular defense protection. Nrf2/ARE pathway plays a key role in the anti-inflammatory, antitumor, neuroprotective, and anti-apoptotic effects. Drugs targeted on Nrf2 are expected to be used in the treatment of several diseases such as multiple sclerosis, diabetes, neurodegenerative diseases, and tumors; Some new drugs such as dimethyl fumarate and Bardoxolone have advanced into late clinical phase. This paper introduces the relationship between Nrf2/ARE pathway and diseases as well as the development of drugs targeted on it.
[中图分类号]
[基金项目]
国家重大新药创制专项(2011ZX09401-009)