Conjugation approaches for peptide-mediated delivery of oligonucleotides therapeutics

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Oligonucleotide-based agents are versatile biomolecules that modulate gene expression. The last decade has seen the emergence of oligonucleotide-based tools for biochemical investigations. Importantly, several oligonucleotide-based drugs and vaccines are currently used for various therapeutic applications ranging from anti-inflammatory and anti-viral agents to those used in cardiovascular, ophthalmic, and neuro-muscular disorders. Despite a broad range of applications, achieving efficient oligonucleotide delivery remains a major limitation. A possible solution is to conjugate cell-penetrating peptides with oligonucleotides. This review provides an overview of chemical strategies used to synthesise peptide-oligonucleotide conjugates. The merits and liabilities of these strategies are discussed in the context of synthetic efficiency, and bio-reversible and -irreversible linkages.

Original languageEnglish
Pages (from-to)24-33
Number of pages10
JournalAustralian Journal of Chemistry
Issue number2
Publication statusPublished - 2022


  • 2-cyanoisoicotinamide (CINA) linkage
  • Click chemistry
  • Conjugation
  • Drug delivery
  • Oligonucleotide
  • Peptide
  • Peptide nucleic acids
  • Thiol-maleimide conjugation

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