化学合成的HIV-1逆转录酶和整合酶双靶点抑制剂研究进展  

Advances on chemically synthesized dual inhibitors of HIV-1 reverse transcriptase and integrase

作　　者：康家雄 朱江[2] 李爱秀[1,3] 肖泽云 李凯[1] KANG Jia-xiong;ZHU Jiang;LI Ai-xiu;XlAO Ze-yun;LI Kai(Drug Design Laboratory of Department of Basic Courses,Logistics University of PAP,Tianjin 300309,Chin)

机构地区：[1]武警后勤学院基础部药物设计实验室,天津300309 [2]武警后勤学院卫勤系,天津300309 [3]天津市职业与环境危害防制重点实验室,天津300309

出　　处：《武警后勤学院学报（医学版）》2018年第2期169-176,共8页Journal of Logistics University of PAP（Medical Sciences）

基　　金：国家自然科学基金项目(81241114;30472166);天津市科技攻关计划重点科技攻关专项基金资助项目(06YFGZSH07000);武警后勤学院研究生创新课题(WHYC201605)

摘　　要：近年来,单组分多靶点抗Ⅰ型人类免疫缺陷病毒(human immunodeficiency virus type 1,HIV-1)药物的研发成为热点,已发现的多靶点抑制剂以针对HIV-1逆转录酶(reverse transcriptase,RT)和整合酶(integrase,IN)的双靶点抑制剂居多,特别是作用于非核苷类逆转录酶抑制剂(non-nucleoside reverse transcriptase inhibitor,NNRTI)作用位点和IN活性位点的双靶点抑制剂[简写为:RT(NNRTI)/IN]种类繁多,现将对其中化学合成的HIV-1 RT(NNRTI)/IN双靶点抑制剂研究进展进行综述。Recently, the research and development of single component multi-target anti-HIV-1 drugs has become a hot topic. Among the multi-target inhibitors that have been found, the dual inhibitors of HIV-1 reverse transcriptase（RT） and integrase（IN） occupy the dominant position, especially the dual inhibitors, abbreviated RT（NNRTI）/IN, which target non-nucleoside reverse transcriptase inhibitors（NNRTI） binding pocket and active site of integrase, are diverse kinds. This review summarizes the advances on chemically synthesized HIV-1 RT（NNRTI）/IN.

关 键 词：Ⅰ型人类免疫缺陷病毒 逆转录酶 整合酶 双靶点抑制剂 

分 类 号：R914[医药卫生—药物化学]