HIV-1 entry – an expanding portal for drug discovery

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• 作者：Blair ; Wade S. ; Lin ; Pin-Fang ; Meanwell ; Nicholas A. ; Wallace ; Owen B.
• 关键词：Virology ; Drug discovery ; HIV-1 ; Entry ; Fusion ; Envelopes ; gp120 gp41 ; CD4 co-receptors ; CCR5 ; CXCR4 inhibitors
• 刊名：Drug Discovery Today
• 出版年：2000
• 出版时间：May 1, 2000
• 年：2000
• 卷：5
• 期：5
• 页码：183-194
• 全文大小：304 K

文摘

The advent of highly active antiretroviral therapy (HAART)–combinations of protease and reverse transcriptase inhibitors–provided a potent and clinically effective method of suppressing viral load in HIV-1- infected individuals. However, although initially successful, a broader clinical experience has revealed limitations in this therapeutic regimen, with up to 40 % of treated individuals ultimately failing to sustain control over viral replication. Significant advances in understanding the process by which HIV-1 enters host cells have brought into clear focus a target for drug discovery not represented in the current clinical armamentarium. In this article, the mechanism of HIV-1 entry is reviewed in the context of representative antiviral agents that interfere with key steps in this process.