title: A cyclic PNA-based compound targeting domain IV of HCV IRES RNA inhibits in vitro IRES-dependent translation.
abstract: A cyclic molecule 1 constituted by a hepta-peptide nucleic acid sequence complementary to the apical loop of domain IV of hepatitis C virus (HCV) internal ribosome entry site (IRES) RNA has been prepared via a 'mixed' liquid-phase strategy, which relies on easily available protected PNA and poly(2-aminoethylglycinamide) building blocks. This compound 1 has been elaborated to mimic 'loop-loop' interactions. For comparison, its linear analog has also been investigated. Although preliminary biological assays have revealed the ability of 1 to inhibit in vitro the HCV IRES-dependent translation in a dose-dependent manner, the linear analog has shown a slightly higher activity.
authors.affiliation: Laboratoire de Chimie Bioorganique UMR-CNRS 6001, Université de Nice-Sophia Antipolis, Parc Valrose, 06108 Nice Cedex, France.
authors.forename: Sergio A
authors.initials: SA
authors.lastname: Caldarelli
authors.forename: Mohamed
authors.initials: M
authors.lastname: Mehiri
authors.forename: Audrey
authors.initials: A
authors.lastname: Di Giorgio
authors.forename: Amaury
authors.initials: A
authors.lastname: Martin
authors.forename: Olivier
authors.initials: O
authors.lastname: Hantz
authors.forename: Fabien
authors.initials: F
authors.lastname: Zoulim
authors.forename: Raphael
authors.initials: R
authors.lastname: Terreux
authors.forename: Roger
authors.initials: R
authors.lastname: Condom
authors.forename: Nadia
authors.initials: N
authors.lastname: Patino
mesh_terms: D016174:Hepacivirus / Q000235:genetics*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D020135:Peptide Nucleic Acids / Q000737:chemistry / Q000187:drug effects*; D014176:Protein Biosynthesis; D012367:RNA, Viral / Q000502:physiology*; D012270:Ribosomes / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D020135:Peptide Nucleic Acids; D012367:RNA, Viral