title: Triple helix-specific ligands.
abstract: A triple helix is formed upon binding of an oligodeoxynucleotide to the major groove of duplex DNA. A benzo[e]pyridoindole derivative (BePI) strongly stabilized this structure and showed preferential binding to a triplex rather than to a duplex. Energy transfer experiments suggest that BePI intercalates within the triple helix. Sequence-specific inhibition of transcription initiation of a specific gene by Escherichia coli RNA polymerase by a triplex-forming oligodeoxynucleotide is strongly enhanced when the triplex is stabilized by BePI. Upon irradiation with ultraviolet light, BePI induces covalent modifications of the target within the triple helix structure.
authors.affiliation: Laboratoire de Biophysique, Institut National de la Santé et de la Recherche Médicale, Paris, France.
authors.forename: J L
authors.initials: JL
authors.lastname: Mergny
authors.forename: G
authors.initials: G
authors.lastname: Duval-Valentin
authors.forename: C H
authors.initials: CH
authors.lastname: Nguyen
authors.forename: L
authors.initials: L
authors.lastname: Perrouault
authors.forename: B
authors.initials: B
authors.lastname: Faucon
authors.forename: M
authors.initials: M
authors.lastname: Rougée
authors.forename: T
authors.initials: T
authors.lastname: Montenay-Garestier
authors.forename: E
authors.initials: E
authors.lastname: Bisagni
authors.forename: C
authors.initials: C
authors.lastname: Hélène
mesh_terms: D001483:Base Sequence; D002243:Carbolines / Q000378:metabolism; D004247:DNA / Q000235:genetics / Q000378:metabolism*; D012321:DNA-Directed RNA Polymerases / Q000235:genetics / Q000378:metabolism; D004926:Escherichia coli / Q000235:genetics*; D006358:Hot Temperature; D066298:In Vitro Techniques; D008024:Ligands; D008969:Molecular Sequence Data; D009693:Nucleic Acid Hybridization; D014158:Transcription, Genetic
chemical_list: D002243:Carbolines; D008024:Ligands; C051802:triplex DNA; D004247:DNA; D012321:DNA-Directed RNA Polymerases