Targeting the HIV-protease in AIDS therapy: a current clinical perspective
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- 作者：Tomasselli ; Alfredo G. ; Heinrikson ; Robert L.
- 关键词：HIV ; AIDS ; Protease ; Protease inhibitor ; Viral resistance ; High throughput screening ; Computer-assisted drug design ; Highly active antiretroviral therapy
- 刊名：Biochimica et Biophysica Acta (BBA)/Protein Structure and Molecular Enzymology
- 出版年：2000
- 出版时间：March 7, 2000
- 年：2000
- 卷：1477
- 期：1-2
- 页码：189-214
- 全文大小：1.40 M
文摘
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.