Document Detail

Polyamide amino acids trimers as TAR RNA ligands and anti-HIV agents.
MedLine Citation:
PMID:  20889349     Owner:  NLM     Status:  In-Process    
Based on a split-and-mix strategy, a library of trimeric Polyamide Amino Acids (PAA) incorporating four different amino acids (Lys, Ala, Arg, and Phe) has been prepared. Screening of the batches for HIV TAR RNA binding in a fluorescent assay allowed the identification of several components that interact with TAR RNA at a micromolar concentration, with a good TAR versus tRNA specificity. Some of these compounds compete efficiently with the association of TAR and Tat protein. In cell cultures, these compounds display a moderate antiviral activity, associated nevertheless with some toxicity. Overall, these results confirm that this new family can be a basis for the design of novel RNA targeting drugs.
Vanessa Bonnard; Lise Pascale; Stéphane Azoulay; Audrey Di Giorgio; Christine Rogez-Kreuz; Karine Storck; Pascal Clayette; Nadia Patino
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-09-07
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  18     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2010 Nov 
Date Detail:
Created Date:  2010-10-18     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  7432-8     Citation Subset:  IM    
Copyright Information:
Copyright © 2010 Elsevier Ltd. All rights reserved.
Laboratoire de Chimie des Molécules Bioactives et des Arômes, UMR 6001 CNRS UNSA, Institut de Chimie de Nice, Université de Nice Sophia Antipolis, 06108 Nice Cedex, France.
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