作　　者： (姚争光）; (张文）; (张万年）; (庄春林）;

机构地区： 蚌埠医学院药学系,安徽蚌埠233030

出　　处： 《中国药物化学杂志》 2017年第4期325-333,共9页

摘　　要： 转录因子E2相关因子2(Nrf2),受Kelch样环氧氯丙烷相关蛋白1(Keap1)蛋白的调控,是细胞氧化应激反应中的关键因子。氧化应激时,Keap1的半胱氨酸残基被修饰,构象改变后导致Nrf2蛋白释放,Nrf2进入细胞核并促进Ⅱ相解毒酶的表达,发挥细胞保护作用;病理条件下,机体无法使Nrf2-Keap1解离,导致疾病发生。近年来,通过非共价修饰作用于Nrf2-Keap1蛋白相互作用界面,成为激活Nrf2防御机制发挥抗氧化防制的重要策略。本文综述了近年来各类Nrf2激活剂的研究进展。 Nuclear factor erythroid-2 related factor 2（ Nrf2） is a pivotal factor of cell oxidative stress that is regulated by Kelch-like ECH-associated protein 1（ Keap1）. Under the condition of oxidative stress,cysteine residues of Keap1 are modified leading to the conformational change and releasing the Nrf2 protein into the nucleus,which promotes the expression of phase Ⅱ enzymes and protect the cells. Under pathological condition,the Nrf2-Keap1 interaction cannot be disrupted. In recent years,non-covalently binding to the Nrf2-Keap1 protein-protein interface is an important strategy to activate Nrf2 and exert antioxidant defense. In this review,several series of Nrf2 activators were summarized.

关 键 词： 蛋白相互作用 抑制剂