表观遗传学药物FK228的药理作用及机制

新型组蛋白去乙酰化酶抑制剂FK228单独用药或与其他药物及方法联合表现出良好的抗肿瘤效应。其作用机制主要是抑制肿瘤细胞内组蛋白去乙酰化酶(HDAC)活性，引起乙酰化组蛋白的积聚,从而发挥抑制肿瘤细胞增殖、诱导细胞周期阻滞、促进细胞凋亡或分化,同时还可阻碍血管生成、抑制转移、逆转耐药性、调节免疫力等作用。FK228还具有治疗炎症、免疫性疾病、视网膜新生血管疾病及神经系统等多种疾病的药理学作用。

Pharmacological activities and mechanisms of epigenetics drug FK228

FK228,a novel histone deacetylase inhibitor,alone or combining with other drugs or methods,has shown a good antitumor effect.The anti-tumour mechanism of FK228 is mainly includes that FK228 inhibits the activity of HDAC and causes the accumulation of histone proteins acetylation sites in tumour cell,which inhibits tumor cell proliferation,induces cell cycle arrest,differentiation and apoptosis,or impedes angiogenesis,tumour metastasis,reverses drug resistance,regulates immune acvities.Recent studies have demonstrated that FK228 can be used in the treatments of inflammatory diseases,autoimmune diseases,retinal neovascularization diseases and nervous system diseases and so on.This article reviewed the recent-year progress of the study on the pharmacological activities and molecular mechanisms of epigenetics drug FK228.