The oxime bond formation as a useful tool for the preparation of oligonucleotide conjugates

Synthetic oligonucleotides are attracting considerable interest as potential therapeutic agents for the selective inhibition of gene expression. The attainment of effective cellular delivery however remains a problem. The conjugation of oligonucleotides to cell penetrating peptides is one of the most promising alternatives, that is being currently investigated to improve the uptake efficiency of oligonucleotides. The synthesis of peptide–oligonucleotide conjugates (POC) is however still a problem. Work from our laboratory has attempted to address the problem of POC synthesis by using the chemoselective oxime bond formation. Herein, we present an account of the work accomplished in our laboratory in the recent past, concerning the conjugation of various reporters to oligonucleotides. .