Branched oligonucleotide-intercalator conjugate forming a parallel stranded structure inhibits HIV-1 integrase. |
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Authors: | P Brodin M Pinskaya E Volkov E Romanova H Leh C Auclair J F Mouscadet M Gottikh |
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Institution: | CNRS-UMR 8532, Institut Gustave Roussy, 39 rue C., Desmoulins, France. |
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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. |
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