RNA as a Target for Drug Design, the Example of Tat-TAR Interaction

Author(s): M. Froeyen, P. Herdewijn.

Journal Name: Current Topics in Medicinal Chemistry

Volume 2 , Issue 10 , 2002

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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

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Article Details

Year: 2002
Page: [1123 - 1145]
Pages: 23
DOI: 10.2174/1568026023393200
Price: $58

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