title: 6-oxocytidine containing oligonucleotides inhibit the HIV-1 integrase in vitro.
abstract: Integration of the proviral DNA into the genome of infected cells is a key step of HIV-1 replication. Integration is catalyzed by the viral enzyme integrase (IN). 6-oxocytidine-containing oligonucleotides were found to be efficient inhibitors of integrase in vitro. The inhibitory effect is sequence-specific and strictly requires the presence of the 6-oxocytidine base. It is due to the impairment of the integrase binding to its substrate and does not involve an auto-structure of the oligonucleotide.
authors.affiliation: UMR 8532, Institut Gustave Roussy, 39 rue Camille Desmoulins, 94805 Villejuif, France.
authors.forename: P
authors.initials: P
authors.lastname: Brodin
authors.forename: M
authors.initials: M
authors.lastname: Pinskaya
authors.forename: U
authors.initials: U
authors.lastname: Parsch
authors.forename: J
authors.initials: J
authors.lastname: Bischerour
authors.forename: H
authors.initials: H
authors.lastname: Leh
authors.forename: E
authors.initials: E
authors.lastname: Romanova
authors.forename: J W
authors.initials: JW
authors.lastname: Engels
authors.forename: M
authors.initials: M
authors.lastname: Gottikh
authors.forename: J F
authors.initials: JF
authors.lastname: Mouscadet
mesh_terms: D002942:Circular Dichroism; D003562:Cytidine / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000494:pharmacology*; D019427:HIV Integrase / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D009841:Oligonucleotides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D019428:HIV Integrase Inhibitors; D009841:Oligonucleotides; C095942:6-oxocytidine; D003562:Cytidine; D019427:HIV Integrase