Efficient synthesis of oligonucleotide-peptide conjugates on large scale.
The conjugation of oligonucleotide phosphorothioates with antennapedia peptide was studied in detail to allow efficient preparation of the conjugates on up to 15 mumol 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.
Doronina
S O
SO
Department of Medicinal Chemistry, Isis Pharmaceuticals, Inc., 2292 Faraday Avenue, Carlsbad, California 92008, USA.
Guzaev
A P
AP
Manoharan
M
M
D009841:Oligonucleotides / Q000138:chemical synthesis* / Q000737:chemistry; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry; D013873:Thionucleotides / Q000737:chemistry
D009841:Oligonucleotides; D010455:Peptides; D013873:Thionucleotides