title: Polyamide amino acids trimers as TAR RNA ligands and anti-HIV agents.
abstract: 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.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.
authors.forename: Vanessa
authors.initials: V
authors.lastname: Bonnard
authors.forename: Lise
authors.initials: L
authors.lastname: Pascale
authors.forename: Stéphane
authors.initials: S
authors.lastname: Azoulay
authors.forename: Audrey
authors.initials: A
authors.lastname: Di Giorgio
authors.forename: Christine
authors.initials: C
authors.lastname: Rogez-Kreuz
authors.forename: Karine
authors.initials: K
authors.lastname: Storck
authors.forename: Pascal
authors.initials: P
authors.lastname: Clayette
authors.forename: Nadia
authors.initials: N
authors.lastname: Patino
mesh_terms: D000595:Amino Acid Sequence; D000596:Amino Acids / Q000737:chemistry*; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D031541:Fluorescence Resonance Energy Transfer; D016325:HIV Long Terminal Repeat; D008024:Ligands; D009757:Nylons / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D012367:RNA, Viral / Q000737:chemistry* / Q000378:metabolism; D054322:tat Gene Products, Human Immunodeficiency Virus / Q000737:chemistry / Q000378:metabolism
chemical_list: D000596:Amino Acids; D019380:Anti-HIV Agents; D008024:Ligands; D009757:Nylons; D012367:RNA, Viral; D054322:tat Gene Products, Human Immunodeficiency Virus