组蛋白去乙酰化酶抑制剂具有众多生物学功能,如抗肿瘤、抗真菌、抗病毒、抗炎症等作用,其对肿瘤细胞表现出强大的功能。FK228作为一种新型组蛋白去乙酰化酶抑制剂,因其特殊的缩酯环肽结构,可有效透过细胞膜,通过抑制组蛋白去乙酰化酶而显示良好的抗肿瘤活性,同时仅引起轻微的不良反应,已经被美国FDA批准用于治疗外周及皮肤T-细胞淋巴瘤。全文就FK228在抗肿瘤方面取得的研究进展作一综述。 Histone deacetylase inhibitors have a number of biological functions, such as anti-tumor, anti-fungal, anti-virus, anti-inflammatory effect, which showed a powerful function of tumor cells. As a novel histone deacetylase inhibitor, FK228, due to its special tricyclic cyclopeptide structure, can effectively penetrate the cell membrane and show good anti-tumor activity by inhibiting histone deacetylase while causing only mild Adverse reactions have been approved by the U.S. FDA for the treatment of peripheral and cutaneous T-cell lymphomas. The article reviews the progress of FK228 in anti-tumor research.