基于Bromodomains靶体的小分子抑制剂的合成进展  

Progress on Synthesis of Small Molecule Inhibitor Based on the Target of Bromodomains

作　　者：黄一波[1,2] 管丹[1] 徐进杰[1] 王亮[2,3] 

机构地区：[1]常州工程职业技术学院制药与生物工程技术系,江苏常州213164 [2]江苏省精细化工重点实验室,江苏常州213164 [3]常州大学石油与化工学院,江苏常州213164

出　　处：《化学试剂》2014年第11期997-1002,1038,共7页Chemical Reagents

基　　金：常州市应用基础类研究计划资助项目(CJ2013-0003);江苏省精细化工重点实验室开放课题(KF1304)

摘　　要：Bromodomains是包含110个氨基酸的蛋白质功能结构域,可选择性识别组蛋白末端乙酰赖氨酸位点,参与表观遗传基因的读取和调控,影响一些疾病的发生。而基于Bromodomains靶体的小分子抑制剂的合成与应用,成为药物化学领域的研究热点。因此,对近三年该领域的合成进展进行归纳和总结,可为抗癌药物的发现提供研究思路。Bromodomains are specific functional protein domains containing more than 100 amino acids,which could selectively recognize acetylated lysine at the end of histones. In the meanwhile,Bromodomains are involved in the reading and regulating epigenetic gene resulting in some diseases. Therefore,the synthesis and application of small molecule inhibitor based on Bromodomains,have become a hot topic in the pharmaceutical chemistry. Herein,the current progress has been summarized in near three years,which can provide ideas and strategies for anti-cancer drug discovery.

关 键 词：Bromodomains 小分子抑制剂 表观遗传基因 合成 

分 类 号：O626[理学—有机化学]