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JAC Advance Access originally published online on June 24, 2005
Journal of Antimicrobial Chemotherapy 2005 56(2):270-272; doi:10.1093/jac/dki208
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© The Author 2005. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For Permissions, please e-mail: journals.permissions@oupjournals.org

Leading article

Cyclotriazadisulfonamides: promising new CD4-targeted anti-HIV drugs

Kurt Vermeire* and Dominique Schols

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

* Corresponding author. Tel: +32-16-33-73-41; Fax: +32-16-33-73-40; E-mail: kurt.vermeire{at}rega.kuleuven.ac.be

It is imperative to continue efforts to identify novel effective therapies that can assist in containing the spread of HIV. Recently acquired knowledge about the HIV entry process points to new strategies to block viral entry. For most HIV strains, the successful infection of their target cells is mainly dependent on the presence of the CD4 surface molecule, which serves as the primary virus receptor. The attachment of the viral envelope to this cellular CD4 receptor can be considered as an ideal target with multiple windows of opportunity for therapeutic intervention. Therefore, drugs that interfere with the CD4 receptor, and thus inhibit viral entry, may be promising agents for the treatment of AIDS. The CD4-targeted HIV entry inhibitors cyclotriazadisulfonamides represent a novel class of small molecule antiviral agents with a unique mode of action. The lead compound, CADA, specifically interacts with the cellular CD4 receptor and is active against a wide variety of HIV strains at submicromolar levels when evaluated in different cell-types such as T cells, monocytes and dendritic cells. Moreover, a strict correlation has been demonstrated between anti-HIV activity and CD4 interaction of about 20 different CADA analogues. In addition, CADA acted synergistically in combination with all other FDA-approved anti-HIV drugs as well as with compounds that target the main HIV co-receptors. In this article, the characteristics of cyclotriazadisulfonamide compounds are presented and the possible application of CADA as a microbicide is also discussed.

Keywords: HIV entry , CADA , CD4 receptor , down-modulation , microbicides


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This article has been cited by other articles:


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K. Vermeire, K. Van Laethem, W. Janssens, T. W. Bell, and D. Schols
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