title: Branched oligonucleotide-intercalator conjugate forming a parallel stranded structure inhibits HIV-1 integrase.
abstract: Integration of a DNA copy of the HIV-1 genome into chromosomal DNA of infected cells is a key step of viral replication. Integration is carried out by integrase, a viral protein which binds to both ends of viral DNA and catalyses reactions of the 3'-end processing and strand transfer. A 3'-3' branched oligonucleotide functionalised by the intercalator oxazolopyridocarbazole at each 5'-end was found to inhibit integration in vitro. We show that both a specific (G,A) sequence and the OPC intercalating agent contribute to the capability of the branched oligonucleotide to form a parallel stranded structure responsible for the inhibition.
authors.affiliation: CNRS-UMR 8532, Institut Gustave Roussy, 39 rue C., Desmoulins, France.
authors.forename: P
authors.initials: P
authors.lastname: Brodin
authors.forename: M
authors.initials: M
authors.lastname: Pinskaya
authors.forename: E
authors.initials: E
authors.lastname: Volkov
authors.forename: E
authors.initials: E
authors.lastname: Romanova
authors.forename: H
authors.initials: H
authors.lastname: Leh
authors.forename: C
authors.initials: C
authors.lastname: Auclair
authors.forename: J F
authors.initials: JF
authors.lastname: Mouscadet
authors.forename: M
authors.initials: M
authors.lastname: Gottikh
mesh_terms: D001483:Base Sequence; D002227:Carbazoles / Q000378:metabolism; D002942:Circular Dichroism; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000378:metabolism*; D008969:Molecular Sequence Data; D009841:Oligonucleotides / Q000378:metabolism / Q000494:pharmacology; D011485:Protein Binding; D013696:Temperature; D014466:Ultraviolet Rays
chemical_list: D002227:Carbazoles; D019428:HIV Integrase Inhibitors; D009841:Oligonucleotides; C061416:oxazolopyridocarbazole; D019427:HIV Integrase