Document Detail


Polyamide amino acids trimers as TAR RNA ligands and anti-HIV agents.
MedLine Citation:
PMID:  20889349     Owner:  NLM     Status:  In-Process    
Abstract/OtherAbstract:
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.
Authors:
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.
Affiliation:
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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