6-oxocytidine containing oligonucleotides inhibit the HIV-1 integrase in vitro.
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.
Brodin
P
P
UMR 8532, Institut Gustave Roussy, 39 rue Camille Desmoulins, 94805 Villejuif, France.
Pinskaya
M
M
Parsch
U
U
Bischerour
J
J
Leh
H
H
Romanova
E
E
Engels
J W
JW
Gottikh
M
M
Mouscadet
J F
JF
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*
D019428:HIV Integrase Inhibitors; D009841:Oligonucleotides; C095942:6-oxocytidine; D003562:Cytidine; D019427:HIV Integrase