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化学进展  2013 

Nrf2通路在肿瘤化学预防中的研究进展

DOI: 10.7536/PC130718, PP. 1544-1552

Keywords: Nrf2,抗氧化反应元件,化学预防

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Abstract:

转录因子E2相关因子2(Nrf2)通过与抗氧化反应元件(ARE)结合正向调控Ⅱ相解毒酶基因、抗氧化酶基因及药物转运泵基因等靶基因的表达。在正常条件下Nrf2与Kelch样环氧氯丙烷相关蛋白(KEAP1)在细胞质中结合导致其被蛋白酶体降解;当细胞受亲电试剂或活性氧进攻时,Nrf2蛋白水平增加并移位于细胞核,激活多种细胞保护基因的转录。近年来Nrf2通路在癌细胞中的作用越来越受关注,本文概括了Nrf2/ARE信号通路的调控机制,讨论了Nrf2在肿瘤化学预防和癌症发生双方面的作用,归纳了影响Nrf2通路小分子化合物的筛选方法和Nrf2抑制剂的研究进展。

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