EFFICIENT SYNTHESIS OF OLIGONUCLEOTIDE-PEPTIDE CONJUGATES ON LARGE SCALE

Abstract

The conjugation of oligonucleotide phosphorothioates with antennapedia peptide was studied in detail to allow efficient preparation of the conjugates on up to 15 μmol scale. Under optimized conditions, the use of oligonucleotides and the peptide in an equimolecular ratio gave the desired conjugates in more than 60% isolated yield.

ACKNOWLEDGEMENTS

We thank Dr. Len Cummins for LC-MS analyses.