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组蛋白去乙酰化酶抑制剂(HDACi)是一类新的化疗药物,能够有效抑制组蛋白去乙酰化酶的活性,促进组蛋白及非组蛋白的乙酰化修饰,在转录和翻译后修饰水平调控肿瘤靶蛋白及凋亡相关蛋白的表达和降解,活化凋亡信号通路,诱导肿瘤细胞凋亡。HDACi抑制抗氧化蛋白的表达,提高细胞内活性氧的水平,引起细胞的氧化损伤。因此,氧化损伤诱导的细胞凋亡也是HDACi杀伤肿瘤细胞的重要机制。HDACi诱导细胞凋亡机制的发现将进一步促进HDACi在临床治疗中的应用。
Histone Deacetylase Inhibitors (HDACi) is a new class of chemotherapeutic drugs that can effectively inhibit the activity of histone deacetylases, promote the acetylation of histones and non-histones, and regulate transcription and post-translational modifications. Regulates the expression and degradation of tumor target proteins and apoptosis-related proteins, activates apoptosis signaling pathways, and induces tumor cell apoptosis. HDACi inhibits the expression of anti-oxidation proteins, increases the level of reactive oxygen species in cells, and causes oxidative damage to cells. Therefore, oxidative injury-induced apoptosis is also an important mechanism of HDACi killing tumor cells. The discovery of the mechanism of apoptosis induced by HDACi will further promote the application of HDACi in clinical treatment.