title: Cyclic PNA-based compound directed against HIV-1 TAR RNA: modelling, liquid-phase synthesis and TAR binding.
abstract: A cyclic molecule including a hexameric PNA sequence has been designed and synthesized in order to target the TAR RNA loop of HIV-1 through the formation of a "kissing complex". For comparison, its linear analogue has also been investigated. The synthesis of the cyclic and linear PNA has been accomplished following a liquid-phase strategy using mixed PNA and fully N-protected (aminoethylglycinamide) fragments. The interactions of this cyclic PNA and its linear analogue with TAR RNA have been studied and the results indicate clearly that no interaction occurs between the cyclic antisense PNA and TAR RNA, whereas a tenuous interaction has been detected with its linear PNA analogue.
authors.affiliation: Laboratoire de Chimie Bioorganique, UMR UNSA-CNRS 6001, Faculté des Sciences, Université de Nice-Sophia Antipolis, 06108 Nice Cédex 2, France.
authors.forename: Geoffrey
authors.initials: G
authors.lastname: Depecker
authors.forename: Nadia
authors.initials: N
authors.lastname: Patino
authors.forename: Christophe
authors.initials: C
authors.lastname: Di Giorgio
authors.forename: Raphael
authors.initials: R
authors.lastname: Terreux
authors.forename: Daniel
authors.initials: D
authors.lastname: Cabrol-Bass
authors.forename: Christian
authors.initials: C
authors.lastname: Bailly
authors.forename: Anne-Marie
authors.initials: AM
authors.lastname: Aubertin
authors.forename: Roger
authors.initials: R
authors.lastname: Condom
mesh_terms: D003500:Cyclization; D015195:Drug Design; D016325:HIV Long Terminal Repeat; D015497:HIV-1 / Q000235:genetics*; D006801:Humans; D008958:Models, Molecular; D009696:Nucleic Acids / Q000138:chemical synthesis; D009712:Nucleotides, Cyclic / Q000138:chemical synthesis; D009757:Nylons / Q000138:chemical synthesis / Q000494:pharmacology; D012367:RNA, Viral / Q000737:chemistry / Q000378:metabolism; D044366:Transition Temperature
chemical_list: D009696:Nucleic Acids; D009712:Nucleotides, Cyclic; D009757:Nylons; D012367:RNA, Viral