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Inhibitors of HIV Infection via the Cellular CD4 Receptor

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Recent advances in our understanding of cellular and molecular mechanisms of viral penetration of the target cell have provided the basis for novel chemotherapy and prophylaxis of HIV-1 infections. This knowledge has been successfully applied to the development of inhibitors that target discrete steps of the entry process. Interesting approaches for prevention of HIV-1 entry include the use of small-molecule inhibitors, natural ligands and/or monoclonal antibodies that interfere with gp120/CD4 interaction. Other compounds acting by novel mechanisms have recently been identified as anti-HIV agents and seem worthy of further preclinical development. Of particular interest in this regard are cyclotriazadisulfonamide (CADA) compounds, which down-modulate the cellular receptor, CD4. A series of analogues of 9-benzyl-3-methylene- 1,5-di-p-toluenesulfonyl-1,5,9-triazacyclododecane (CADA) has been synthesized and tested for CD4 downmodulation and anti-HIV activity. Some derivatives proved to be highly effective in decreasing cellular CD4 and in acting as HIV entry inhibitors. Three-dimensional quantitative structure-activity relationship (3DQSAR) studies correlating molecular features with potency have been used to produce a computational model. This model can be used to design more potent CD4 down-modulating drugs for HIV therapy and prophylaxis. This review summarizes the results of recent studies relating to inhibitors of HIV infection via CD4 and discusses the therapeutic potential of targeting this cellular receptor. Special attention is given to our own work on small-molecule HIV entry inhibitors endowed with CD4 down-modulating properties.
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Keywords: CADA; CD4; HIV entry; Human immunodeficiency virus; QSAR; down-regulation; entry inhibitor; structure activity relationship

Document Type: Research Article

Affiliations: Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B- 3000 Leuven, Belgium.

Publication date: 2006-03-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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