6-oxocytidine containing oligonucleotides inhibit the HIV-1 integrase in vitro |
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Authors: | Brodin P Pinskaya M Parsch U Bischerour J Leh H Romanova E Engels J W Gottikh M Mouscadet J F |
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Institution: | UMR 8532, Institut Gustave Roussy, 39 rue Camille Desmoulins, 94805 Villejuif, France. |
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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. |
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