Department of Biochemistry and Molecular Genetics, University of Illinois, Chicago, IL 60607, USA.
Trends Microbiol. 2011 Apr;19(4):191-7. doi: 10.1016/j.tim.2011.02.001. Epub 2011 Mar 4.
The HIV envelope proteins glycoprotein 120 (gp120) and glycoprotein 41 (gp41) play crucial roles in HIV entry, therefore they are of extreme interest in the development of novel therapeutics. Studies using diverse methods, including structural biology and mutagenesis, have resulted in a detailed model for envelope-mediated entry, which consists of multiple conformations, each a potential target for therapeutic intervention. In this review, the challenges, strategies and progress to date for developing novel entry inhibitors directed at disrupting HIV gp120 and gp41 function are discussed.
HIV 包膜蛋白糖蛋白 120(gp120)和糖蛋白 41(gp41)在 HIV 进入中起着至关重要的作用,因此它们是新型治疗药物开发的极感兴趣的目标。使用多种方法(包括结构生物学和诱变)的研究产生了一个详细的包膜介导进入模型,该模型由多个构象组成,每个构象都是治疗干预的潜在目标。在这篇综述中,讨论了开发针对破坏 HIV gp120 和 gp41 功能的新型进入抑制剂所面临的挑战、策略和迄今取得的进展。