Advances in chemical synthesis of dual inhibitors of HIV integrase and ribonuclease H
10.16438/j.0513-4870.2019-0295
- VernacularTitle:化学合成类HIV整合酶和核糖核酸酶H双靶点抑制剂的研究进展
- Author:
Jia-xiong KANG
1
;
Jiang ZHU
2
;
Ai-xiu LI
3
;
Yu-rui JIN
4
Author Information
1. Drug Design Laboratory of the Basic Courses Department, Logistics University of PAP, Tianjin 300309, China; Department of Health Service, Logistics University of PAP, Tianjin 300309, China
2. Department of Health Service, Logistics University of PAP, Tianjin 300309, China
3. Drug Design Laboratory of the Basic Courses Department, Logistics University of PAP, Tianjin 300309, China; Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazard, Tianjin 300309, China
4. Drug Design Laboratory of the Basic Courses Department, Logistics University of PAP, Tianjin 300309, China
- Publication Type:Research Article
- Keywords:
human immunodeficiency virus;
integrase;
ribonuclease H;
ual inhibitors
- From:
Acta Pharmaceutica Sinica
2019;54(8):1392-1401
- CountryChina
- Language:Chinese
-
Abstract:
Antiretroviral therapy has been used for treating AIDS with 31 single-target anti-HIV drugs currently on market. Searching for safe and effective of novel anti-HIV drugs remains a challenge worldwide. Multi-targets single-structure compounds referred to as designed multiple ligands (DMLs) have become a hot topic of producing anti-HIV drugs recently due to reduction in the likelihood of drug resistance, simplified dosing and improved patient adherence. Integrase (IN) and ribonuclease H (RNase H) are two indispensable enzymes in HIV republication, therefore are two important targets for developing anti-HIV drugs. Recently, diverse dual inhibitors of HIV IN and RNase H (IN/RNase H) have been developed via rational drug design and screening. This review summarizes the advances in chemically synthesized dual inhibitors of HIV IN/RNase H to provide the information for developing multi-targets anti-HIV drugs.