组蛋白去乙酰化酶抑制剂联合用药研究进展  

Research advances on histone deacetylase inhibitor combination therapy

作　　者：吕子强[1] 吕紫阳 马成华[3] 马晓成[1] 马小罕 涂志[1] 

机构地区：[1]西北民族大学第一临床医学院 [2]西北民族大学医学院 [3]兰州大学口腔医学院

出　　处：《中国临床药理学与治疗学》2016年第5期579-585,共7页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家科技支撑计划课题(2011BAI05B05)

摘　　要：组蛋白去乙酰化酶抑制剂(HDACi)是一类新型发展起来的抗肿瘤药物,通过调节核小体结构控制抑癌基因表达而发挥抗肿瘤的作用。近年来对具有去乙酰化酶(HDACs)抑制活性化合物的报道越来越少,对HDACi与作用于其他靶点的抗肿瘤药物的联合应用研究逐年增多,并且取得了一定的成就。本文重点介绍了HDACi与细胞毒药物、细胞分化诱导剂全反式维甲酸、DNA去甲基抑制剂(DNMT-i)、蛋白酶体抑制剂、细胞周期DNA修复抑制剂、蛋白酶体抑制剂等的抗肿瘤机制以及联合应用所取得的成绩,并对抗肿瘤药物的研究和发展作出了展望。HDACi is a new developed class of anticancer drugs which can play a role of anti-tumor by adjusting the nucleosome structure to control the expression of the tumor suppressor gene.Recently,the reported compounds which inhibit HDACs activities were fewer and fewer.The reports about the HDACi combined with other antitumor drugs that aimed at the other target points had been increased gradually.This work introduced the antitumor mechanism and achievements of HDACi in combination with the cytotoxic drugs,ATRA,DNMT-Ⅰ,proteasome inhibitor,DNA repair inhibitors,proteasome inhibitors,etc.The expectation about the research and development of the antineoplastic drugs was also been made in this paper.

关 键 词：组蛋白乙酰酶抑制剂 联合治疗 抗肿瘤 

分 类 号：R979.1[医药卫生—药品]