去乙酰基化酶及其抑制剂在癌症研究中的应用  

Histone deacetylase and application of its inhibitors in cancer research

作　　者：王宇瑄 钟同同 柏瑞芳 崔艳[1] WANG Yuxuan;ZHONG Tongtong;BAI Ruifang;CUI Yan(School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2020年第9期841-846,共6页Journal of Shenyang Pharmaceutical University

基　　金：沈阳药科大学大学生创新创业项目(201910163019)。

摘　　要：目的对去乙酰基化酶(histone deacetylases,HDACs)及其抑制剂(histone deacetylase inhibitors,HDACis)在癌症中的应用进行综述。方法检索国内外近几年关于HDACs及HDACis的文章,从它们的分类、作用机制和功能特点出发结合其与癌症发生发展和治疗的关系对文献进行整理和综述。结果HDACs分为四型——I、II、III和IV型,HDACis分为泛抑制剂和选择性抑制剂。HDACs和HDACis均通过调节细胞内的分子反应,影响细胞的增殖、代谢、修复与凋亡,进而达到导致或治疗癌症的目的。结论确定HDACis抑制肿瘤的具体分子机制,并且明确未来癌症治疗的主要研究方向是开发细胞毒副作用较低的选择性抑制剂。Objective To summarize the histone deacetylases(HDACs)and the application of its inhibitors(HDACis)in cancer researches.Methods Based on the classification,mechanism,and functional characteristics of HDACs and its inhibitors,research articles were retrieved and summarized according to the tumorigenesis,tumor progression and cancer treatment.Results HDACs could be classified into four classes,and HDACis could be classified into pan HDACis and selective HDACis.HDACs and HDACis brought the alternation of molecular reaction to the cell which result in the regulation of cell proliferation,differentiation,apoptosis and other cellular process.These processes led to carcinogenesis or treatment of cancer.Conclusion Specific clarification of HDACis treatment mechanism and development of selective HDACis inhibitors with low cytotoxic side effects will be the main direction of cancer therapy.

关 键 词：去乙酰基化酶 去乙酰基化酶抑制剂 癌症 表观遗传 组蛋白 

分 类 号：R96[医药卫生—药理学]