刍议组蛋白去乙酰化酶的结构分类与功能调控  

Discussion on structure classification and regulation function of histone deacetylase

作　　者：王志鹏 张璇[4] 蒋振雄[5,6] 车子良 马新雨 WANG Zhipeng;ZHANG Xuan;JIANG Zhenxiong;CHE Ziliang;MA Xinyu(Division of Genetics,Department of Medicine,Brigham and Women's Hospital,Department of Biological Chemistry and Molecular Pharmacology,Harvard Medical School,Boston 02115,USA;Department of Chemistry,Texas A&M University,College Station 77840,USA;Department of Chemistry,Tsinghua University,Beijing 100084,China;School of Life Sciences,Tsinghua University,Beijing 100084,China;Department of Plant and Pathology and Microbiology,Texas A&M University,College Station 77840,USA;Department of Biology,Texas A&M University,College Station 77840,USA)

机构地区：[1]Division of Genetics,Department of Medicine,Brigham and Women's Hospital,Department of Biological Chemistry and Molecular Pharmacology,Harvard Medical School,Boston 02115,USA [2]Department of Chemistry,Texas A&M University,College Station 77B40,USA [3]清华大学化学系,北京100084 [4]清华大学生命学院,北京100084 [5]Department of Plant and Pathology and Microbiology,Texas A&M University,College Station 77840,USA [6]Department of Biology,Texas A&M University,College Station 77840,USA

出　　处：《生命的化学》2020年第12期2151-2161,共11页Chemistry of Life

摘　　要：赖氨酸乙酰化是一类典型的组蛋白翻译后修饰,受到组蛋白乙酰转移酶(HAT)和组蛋白去乙酰化酶(HDAC)的共同精细调控。尽管HDAC一直是学科研究的前沿问题,但在国内科研综述或教学中缺乏相关内容的阐述。本文从HDAC的发现历史和去除乙酰化的机制入手,在现有对HDAC分类的基础上,依次概述了4类HDAC的基本结构特征和生物功能。此外,本文还分析了针对不同HDAC的抑制剂及其在医学药学中的应用,旨在为相关的靶点研究及教学工作提供参考。Lysine acetylation is a typical type of histone post-transcription m odification,w hich is sophisticatedly regulated by HATs and HDAC.Although HDAC has always been the frontier of subject research,there is a lack of elaboration of relevant content in Chinese scientific reviews for research or education.This review starts from the discovery history and mechanism of acetylation removal,summarizing the basic structural characteristics and biological functions of four types of HDAC based on the existing classification of HDAC.Moreover,we also hope to analyze current inhibitor development for different HDAC and their clinic and pharmaceutical applications,in order to provide a reference for relevant target research and teaching work.

关 键 词：赖氨酸乙酰化 去乙酰化酶 组蛋白去乙酰化酶抑制剂 

分 类 号：Q75[生物学—分子生物学]