SYNTHESIS OF PEPTIDE-OLIGONUCLEOTIDE PHOSPHOROTHIOATE CONJUGATES BY CONVERGENT OR STEPWISE SOLID-PHASE STRATEGIES

Abstract

A convergent strategy was employed to link eight 10–27-mer peptides to oligonucleotide phosphorothioates, resulting in twenty-six various conjugates. A stepwise synthesis strategy for the preparation of peptide-oligonucleotide phosphorothioate conjugates, employing Fmoc peptide chemistry, was developed and applied to the synthesis of four conjugates. Three of these conjugates contained either a 10 or 16-mer peptide, incorporating either 2 or 3 arginine residues, respectively.

ACKNOWLEDGMENTS

Financial support from the Technology Development Center of Finaland is gratefully acknowledged.