Versatile synthesis of oligodeoxyribonucleotide-oligospermine conjugates |
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Authors: | Voirin Emilie Behr Jean-Paul Kotera Mitsuharu |
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Affiliation: | Polyplus-transfection SA, Bioparc, Boulevard S. Brandt, BP90018, 67401 Illkirch, France. |
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Abstract: | A protocol for the rapid, automated synthesis of oligospermine-oligonucleotide sequences is described. To this end, a protected spermine phosphoramidite derivative was synthesized in six steps from spermine and used as the fifth synthon in an oligonucleotide synthesizer. Parameters were optimized to reach greater than 95% coupling yields. Cationic oligonucleotides show enhanced hybridization and strand invasion properties, and hence are an alternative to conventional oligonucleotides for molecular biology, diagnostic and potential therapeutic applications. A multi-gram-scale synthesis of the spermine phosphoramidite allowing several hundred coupling steps takes 2-3 weeks. Oligonucleotide synthesis and purification takes approximately 3 d. |
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