Low molecular weight oligonucleotides have been discovered to have potential use for gene therapy by selectively
inhibiting the expression of certain genes. Chemical conjugation of functional peptides to oligonucleotides can introduce
desired properties to the oligonucleotides, such as cell-specific delivery, cellular uptake efficiency, and/or intracellular
distribution. In this paper, targeting peptides are conjugated to antisense interleukin-6 via a copper (I) catalyzed
alkyne-azide cycloaddition click reaction. A simple and reproducible solution-phase conjugation procedure was investigated.
Oligonucleotide-peptide conjugations were characterized by reverse-phase high-pressure liquid chromatography
and mass spectrometry. The results show that the targeting peptides can be used for targeting delivery of oligonucleotides
using the aforementioned conjugation.
Keywords: Antisense, click chemistry, interleukin-6, peptide-oligonucleotide conjugation, targeting peptides.
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