Abstract
One of the new targets in the battle against HIV-1 infection is the interaction between the viral transactivator and the transactivation response (TAR) element, which is necessary for HIV-1 replication. After an overview of the most recent structural studies of the Tat-TAR system, new TAR-targeted inhibitors are presented in several classes:antisense oligonucleotides, cationic peptides, intercalators and a large class of small RNA binding molecules. The method of library screening of RNA binding ligands in the search for new inhibitors is explained in detail. Inhibition of Tat-TAR interaction is considered as a realistic approach to develop new anti-HIV compounds. The RNA binding molecules in this review also demonstrate that the development of drugs that target RNA will become a feasible goal and that such compounds will be added in the future to the therapeutic arsenal to combat several diseases.
Keywords: tat-tar interaction, hiv-1 infection, rna binding ligands, the tat protein, virus replication, antisense oligonucleotides, library screening
Current Topics in Medicinal Chemistry
Title: RNA as a Target for Drug Design, the Example of Tat-TAR Interaction
Volume: 2 Issue: 10
Author(s): M. Froeyen and P. Herdewijn
Affiliation:
Keywords: tat-tar interaction, hiv-1 infection, rna binding ligands, the tat protein, virus replication, antisense oligonucleotides, library screening
Abstract: One of the new targets in the battle against HIV-1 infection is the interaction between the viral transactivator and the transactivation response (TAR) element, which is necessary for HIV-1 replication. After an overview of the most recent structural studies of the Tat-TAR system, new TAR-targeted inhibitors are presented in several classes:antisense oligonucleotides, cationic peptides, intercalators and a large class of small RNA binding molecules. The method of library screening of RNA binding ligands in the search for new inhibitors is explained in detail. Inhibition of Tat-TAR interaction is considered as a realistic approach to develop new anti-HIV compounds. The RNA binding molecules in this review also demonstrate that the development of drugs that target RNA will become a feasible goal and that such compounds will be added in the future to the therapeutic arsenal to combat several diseases.
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Cite this article as:
Froeyen M. and Herdewijn P., RNA as a Target for Drug Design, the Example of Tat-TAR Interaction, Current Topics in Medicinal Chemistry 2002; 2 (10) . https://dx.doi.org/10.2174/1568026023393200
DOI https://dx.doi.org/10.2174/1568026023393200 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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