以组蛋白去乙酰化酶为靶点的抗肿瘤研究

Research on histone deacetylase as a target for anti-cancer therapy

细胞核内组蛋白乙酰化与去乙酰化失衡可诱发肿瘤.组蛋白去乙酰化酶（HDAC）作用于组蛋白,使其去乙酰化,维系组蛋白乙酰化与去乙酰化的平衡状态,与癌相关基因转录表达、细胞增殖分化及细胞凋亡等过程密切相关.HDAC抑制剂目前是国内外研究的热点,已有十多种HDAC抑制剂用于治疗血液肿瘤和恶性实体瘤,表现出明显的抗肿瘤活性.

The disequilibrium of histone acetylation and deacetylation may cause tumor.Histone deacetylases （HDACs） maintain the equilibrium between histone acetylation and deacetylation by catalyzing the deacetylation of histone.They are related to many regulation processes containing transcription of oncogene,cell proliferation and differentiation,apoptosis and so on.HDACs inhibitors have become the hot field of researches,more than ten different HDACs inhibitors are testing for the treatment of both hematological and solid malignancies and show obvious anti-tumor activity.