Abstract
组蛋白去乙酰化酶(HDACs)参与组蛋白和非组蛋白赖氨酸残基乙酰化和去乙酰化动态平衡过程的调节,它的异常表达与癌症、神经性疾病、炎症、代谢异常等一系列疾病相关。HDAC具有多种亚型,且组织分布及生理功能均有差异,开发亚型选择性HDAC抑制剂可降低其毒副作用,并成为近年来的研究热点,目前已报道多种类型的选择性HDAC抑制剂。本文综述了现阶段选择性HDAC抑制剂的研究进展和潜在适应症。 Histone deacetylases (HDACs) play a crucial role in regulating the balance of acetylation and deacetylation of lysine residues of histones and non-histone proteins, whose overexpression is closely associated with a great variety of cancers, neurological diseases, inflammatory diseases, metabolic disorders and so on. HDAC has lots of subtypes, and the tissue distribution and physiological functions are different, the development of subtype selective HDAC inhibitors can reduce its toxic and side effects, and has become a research hotspot in recent years. Several HDAC inhibitors have been reported so far. This review summarizes the current research progress and potential indications of selective HDAC inhibitors.