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组蛋白乙酰转移酶和组蛋白脱乙酰酶分别催化组蛋白的乙酰化和脱乙酰基反应,调节组蛋白的乙酰化水平,从而调控基因表达。这些过程与恶性肿瘤的发生具有密切的关系。组蛋白脱乙酰酶抑制剂通过增加细胞内组蛋白的乙酰化程度,调节多种基因的表达水平,抑制肿瘤细胞的增殖、诱导细胞分化和凋亡。该文从抑制细胞增殖、诱导细胞分化、诱导细胞凋亡和抗血管形成等4个方面介绍组蛋白脱乙酰酶抑制剂的抗癌机制,并简要介绍它们的分类。
Histone acetyltransferase and histone deacetylase catalyze histone acetylation and deacetylation, respectively, and regulate the acetylation of histones to regulate gene expression. These processes and the occurrence of malignant tumors are closely related. Histone deacetylase inhibitors regulate the expression of multiple genes by increasing the degree of acetylation of intracellular histone proteins, inhibiting the proliferation of tumor cells and inducing cell differentiation and apoptosis. This article describes the anti-cancer mechanisms of histone deacetylase inhibitors from four aspects of inhibiting cell proliferation, inducing cell differentiation, inducing apoptosis and anti-angiogenesis, and briefly introduces their classification.