HIV-1整合酶抑制剂的发展和基因耐药研究  

Development and genetic drug resistance research of HIV-1 integrase inhibitors

作　　者：梁梦然 邹潇白[2] 陈曦[2] LIANG Meng-ran;ZOU Xiao-bai;CHEN Xi(School of Public Health,University of South China,Hengyan,Hunan 421001,China;Hunan Provincial Center for Disease Prevention and Control,Changsha,Hunan 410005,China)

机构地区：[1]南华大学公共卫生学院,湖南衡阳421001 [2]湖南省疾病预防控制中心,湖南长沙410005

出　　处：《中国热带医学》2021年第12期1197-1200,1216,共5页China Tropical Medicine

基　　金：国家科技重大专项(No.2017ZX10201101-002-009)。

摘　　要：整合酶(Integrase,IN)是HIV-1病毒生命周期中最重要的4个酶之一。整合酶抑制剂(integrase inhibitors,INIs)是针对艾滋病患者的新一类抗HIV-1病毒药物,主要针对整合酶发挥作用,阻断病毒基因组整合至人体基因组的过程。相比传统抗病毒治疗药物,INIs上市时间短,耐药屏障高,且人体细胞结构中没有整合酶,毒副作用较小,更有利于患者治疗。但是随着使用人数的增多,不可避免地出现整合酶基因耐药突变。我国目前INIs耐药研究较少,已有研究均参考欧美国家相关数据,但是由于我国流行株以重组亚型为主,与欧美国家B亚型相差较大,因此不能直接借鉴欧美国家的研究结果。有必要深入研究我国流行亚型毒株的整合酶基因型耐药突变情况,同时关注接受INIs治疗患者的耐药情况,弥补我国获得性整合酶耐药研究的空白,为后续大规模临床推广INIs提供数据参考依据。Integrase is one of the four most important enzymes in life cycle of HIV-1 virus.Integrase inhibitors(INIs),a new class of anti-HIV-1 drugs,work primarily on integrases and block the integration of the viral genome into the human genome.Compared with traditional antiviral drugs,INIs are more beneficial to patients because of its shorter time to market,higher drug resistance barrier,less toxicity and side effects.However,drug-resistant mutations in the integrase gene are inevitable as the number of users increases.At present,there are few studies on INIs resistance in China,and all existing studies refer to relevant data in European and American countries.However,prevalent strains in China are mainly recombinant subtypes,which differ greatly from B subtypes in European and American countries.Therefore,we cannot directly learn from the results of European and American countries.It is necessary to study the integrase genotype drug resistance of epidemic HIV-1 subtypes in China,and at the same time pay attention to the drug resistance of INIs patients,which will make up the gap of acquired integrase drug resistance research in China,so as to provides the data reference basis for the follow-up large-scale clinical popularization of INIs.

关 键 词：HIV-1 整合酶抑制剂 基因耐药突变 

分 类 号：R512.91[医药卫生—内科学]