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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。
Novel histone deacetylase inhibitor FK228 alone or in combination with other drugs and methods showed good anti-tumor effect. Its mechanism of action is mainly inhibiting the activity of histone deacetylase (HDAC) in tumor cells, causing the accumulation of acetylated histones, thereby inhibiting tumor cell proliferation, inducing cell cycle arrest, promoting apoptosis or differentiation, and simultaneously Can hinder angiogenesis, inhibition of metastasis, reversal of drug resistance, regulate immunity and so on. FK228 also has the pharmacological effects of treating various diseases such as inflammation, autoimmune diseases, retinal neovascular diseases and nervous system.