Advances in the development of HIV integrase strand transfer inhibitors

被引：17
作者：
Wang, Yue [1 ]
Gu, Shuang-Xi [2 ,3 ]
He, Qiuqin [1 ]
Fan, Renhua [1 ]
机构：
[1] Fudan Univ, Dept Chem, 2005 Songhu Rd, Shanghai 200438, Peoples R China
[2] Wuhan Inst Technol, Sch Chem Engn & Pharm, Key Lab Green Chem Proc, Minist Educ, Wuhan 430205, Peoples R China
[3] Wuhan Inst Technol, Hubei Key Lab Novel Reactor & Green Chem Technol, Wuhan 430205, Peoples R China
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2021年 / 225卷
基金：
中国国家自然科学基金;
关键词：
HIV-1; integrase; Strand transfer inhibitors; Metal chelating; Resistance; ZINC-BINDING DOMAIN; CRYSTAL-STRUCTURE; CATALYTIC DOMAIN; STRUCTURAL BASIS; RALTEGRAVIR; RESISTANT; DOLUTEGRAVIR; ORGANIZATION; ELVITEGRAVIR; REPLICATION;
D O I：
10.1016/j.ejmech.2021.113787
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
HIV-1 integrase (IN) is a key enzyme in viral replication that catalyzes the covalent integration of viral cDNA into the host genome. Currently, five HIV-1 IN strand transfer inhibitors (INSTIs) are approved for clinical use. These drugs represent an important addition to the armamentarium for antiretroviral therapy. This review briefly illustrates the development history of INSTIs. The characteristics of the currently approved INSTIs, as well as their future perspectives, are critically discussed. (C) 2021 Elsevier Masson SAS. All rights reserved.
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页数：10
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