Molecular designing strategies of anti-drug-resistant HIV-1 protease inhibitors
10.3321/j.issn:1000-5048.2009.03.018
- VernacularTitle:抗耐药性HIV-1蛋白酶抑制剂的分子设计策略
- Author:
Youpan MIAO
;
Aixiu LI
;
Tao LIU
;
Kezhu WU
- Publication Type:Journal Article
- Keywords:
anti-drug resistance;
HIV-1 protease inhibitors;
molecular design
- From:
Journal of China Pharmaceutical University
2009;40(3):279-283
- CountryChina
- Language:Chinese
-
Abstract:
HIV-1 protease inhibitors play a very important role in AIDS chemotherapy, but with the rapid emergence of drug resistance as a result of the residue mutation of HIV-1 protease, developing effective protease inhibitors with superior activity against drug-resistant variants is becoming the research hotspot in AIDS drug design. Meanwhile, some molecular designing strategies of anti-drug-resistant HIV-1 protease inhibitors were put forward and applied to develop anti-AIDS drugs. The purpose of the research is introducing these molecular designing strategies to develop potent HIV-1 protease inhibitors to combat drug resistance, including substrate envelope hypothesis, strengthening the binding of inhibitors to HIV-1 protease and searching inhibitors acting in novel sites of HIV-1 protease.
