Nrf2/ARE信號通路是細胞氧化應(yīng)激反應(yīng)中的關(guān)鍵通路，其調(diào)控的下游抗氧化蛋白和Ⅱ相解毒酶在細胞防御保護中發(fā)揮重要作用。現(xiàn)有研究顯示Nrf2/ARE通路在抗炎、抗腫瘤、神經(jīng)保護、抗凋亡等多方面具有重要作用，以Nrf2為靶點的藥物有望用于多發(fā)性硬化、糖尿病、神經(jīng)退行性疾病、腫瘤等多種疾病的治療，其中已有富馬酸二甲酯、巴多克沙龍等多個新藥進入臨床研究階段。就Nrf2/ARE通路與疾病的關(guān)系及以其為靶點的新藥研發(fā)進展做一綜述。

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.

國家重大新藥創(chuàng)制專項（2011ZX09401-009）