A Convenient Solid-Phase Method for the Synthesis of Novel Oligonucleotide-Folate Conjugates

Eugenia V. Kazanova Department of Chemistry and A. N. Belozersky Institute of Physico-Chemical Biology, M. V. Lomonossov Moscow State University, Moscow, Russia

Eugeny M. Zubin Department of Chemistry and A. N. Belozersky Institute of Physico-Chemical Biology, M. V. Lomonossov Moscow State University, Moscow, Russia

Anna V. Kachalova Department of Chemistry and A. N. Belozersky Institute of Physico-Chemical Biology, M. V. Lomonossov Moscow State University, Moscow, Russia

Eugeny M. Volkov Department of Chemistry and A. N. Belozersky Institute of Physico-Chemical Biology, M. V. Lomonossov Moscow State University, Moscow, Russia

Tatiana S. Oretskaya Department of Chemistry and A. N. Belozersky Institute of Physico-Chemical Biology, M. V. Lomonossov Moscow State University, Moscow, Russia

Dmitry A. Stetsenko School of Biomedical and Molecular Sciences, University of Surrey, Guildford, Surrey, United Kingdom

Marina B. Gottikh Department of Chemistry and A. N. Belozersky Institute of Physico-Chemical Biology, M. V. Lomonossov Moscow State University, Moscow, Russia

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Abstract

We describe the preparation of two batches of a polymer support for the incorporation of folic acid into oligonucleotides. The method permits the regioselective attachment of a target nucleic acid sequence through its 3′-end to either the α-or γ-carboxyl group of L-glutamic acid, respectively. The supports have been tested in solid-phase synthesis of oligonucleotide-folate conjugates for cell delivery studies.

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The project was supported by a grant from the EU FP6 (No. LSHC-CT-2004-503036, project PROTHETS) and the President of Russia Grant for Young Scientists (MK-2744.2005.4).

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A Convenient Solid-Phase Method for the Synthesis of Novel Oligonucleotide-Folate Conjugates

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A Convenient Solid-Phase Method for the Synthesis of Novel Oligonucleotide-Folate Conjugates

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