Targeting the HIV-protease in AIDS therapy: a current clinical perspective

被引：121

作者：

Tomasselli, AG ^{[1
]}

Heinrikson, RL ^{[1
]}

机构：

[1] Pharmacia & Upjohn Inc, Dept Prot Sci, Kalamazoo, MI 49001 USA

来源：

BIOCHIMICA ET BIOPHYSICA ACTA-PROTEIN STRUCTURE AND MOLECULAR ENZYMOLOGY | 2000年 / 1477卷 / 1-2期

关键词：

HIV; AIDS; protease; protease inhibitor; viral resistance; high throughput screening; computer-assisted drug design; highly active antiretroviral therapy;

D O I：

10.1016/S0167-4838(99)00273-3

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

This review deals with clinical applications of compounds that inhibit the action of the protease encoded within the genome of human immunodeficiency virus (HIV). The HIV-protease is essential for viral maturation and represents an important therapeutic target in the fight against AIDS. Following a brief overview of the enzyme structure and function, the article focuses on a number of peptide and non-peptide based HIV-protease inhibitors that are in current clinical use. These drugs are discussed both with respect to their efficacy in treatment of AIDS, and to problems related to insurgence of viral resistance and side effects seen to date in patient populations. (C) 2000 Elsevier Science B.V. All rights reserved.

引用

页码：189 / 214

页数：26

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