New method to prepare peptide-oligonucleotide conjugates through glyoxylic oxime formation

J Org Chem. 2004 Nov 26;69(24):8544-6. doi: 10.1021/jo0485177.

Abstract

A new method to prepare peptide-oligonucleotide conjugates through chemoselective glyoxylic oxime linkage is reported. A novel phosphoramidite reagent, readily accessible from serine, was prepared and used in automated DNA synthesis to prepare oligonucleotides carrying a glyoxylic aldehyde functionality at the 5' terminus. This was efficiently coupled to a peptide functionalized with an aminooxy group. The method could be of general use to prepare a broad range of oligonucleotide conjugates.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cross-Linking Reagents / chemical synthesis*
  • Cross-Linking Reagents / chemistry
  • Glyoxylates / chemical synthesis*
  • Glyoxylates / chemistry
  • Oligonucleotides / chemical synthesis*
  • Oligonucleotides / chemistry
  • Oximes / chemical synthesis*
  • Oximes / chemistry
  • Peptide Nucleic Acids / chemical synthesis*
  • Peptide Nucleic Acids / chemistry
  • Peptides / chemical synthesis*
  • Peptides / chemistry
  • Serine / chemistry

Substances

  • Cross-Linking Reagents
  • Glyoxylates
  • Oligonucleotides
  • Oximes
  • Peptide Nucleic Acids
  • Peptides
  • Serine