title: Systematic screening of LNA/2'-O-methyl chimeric derivatives of a TAR RNA aptamer.
abstract: We synthesized and evaluated by surface plasmon resonance 64 LNA/2'-O-methyl sequences corresponding to all possible combinations of such residues in a kissing aptamer loop complementary to the 6-nt loop of the TAR element of HIV-1. Three combinations of LNA/2'-O-methyl nucleoside analogues where one or two LNA units are located on the 3' side of the aptamer loop display an affinity for TAR below 1nM, i.e. one order of magnitude higher than the parent RNA aptamer. One of these combinations inhibits the TAR-dependent luciferase expression in a cell assay.
authors.affiliation: INSERM U869, Institut Européen de Chimie et Biologie, 2 rue Escarpit, Pessac cedex, F-33607, France. c.diprimo@iecb.u-bordeaux.fr
authors.forename: Carmelo
authors.initials: C
authors.lastname: Di Primo
authors.forename: Ivo
authors.initials: I
authors.lastname: Rudloff
authors.forename: Sandrine
authors.initials: S
authors.lastname: Reigadas
authors.forename: Andrey A
authors.initials: AA
authors.lastname: Arzumanov
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Gait
authors.forename: Jean-Jacques
authors.initials: JJ
authors.lastname: Toulmé
mesh_terms: D052157:Aptamers, Nucleotide / Q000737:chemistry* / Q000235:genetics; D001483:Base Sequence; D016325:HIV Long Terminal Repeat; D006367:HeLa Cells; D006801:Humans; D007700:Kinetics; D008156:Luciferases / Q000378:metabolism; D008969:Molecular Sequence Data; D009690:Nucleic Acid Conformation; D009841:Oligonucleotides; D016376:Oligonucleotides, Antisense / Q000032:analysis* / Q000737:chemistry
chemical_list: D052157:Aptamers, Nucleotide; D009841:Oligonucleotides; D016376:Oligonucleotides, Antisense; C477371:locked nucleic acid; D008156:Luciferases