Stepwise solid-phase synthesis of peptide–oligonucleotide phosphorothioate conjugates employing Fmoc peptide chemistry

A straightforward stepwise method for the preparation of peptide–oligonucleotide phosphorothioate conjugates, was developed, based on the highly efficient Fmoc peptide solid phase synthesis, followed by oligonucleotide phosphorothiate chain assembly. The three conjugates synthesized contained 15- or 17-mer oligonucleotide phosphorothioates and 10- or 16-mer peptides, incorporating two or three arginine residues.