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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Conjugation of Peptides to Antisense Interleukin-6 Via Click Chemistry

Author(s): Chang-Fang Wang, Seppo Auriola, Jouni Hirvonen and Helder A. Santos

Volume 21, Issue 10, 2014

Page: [1247 - 1254] Pages: 8

DOI: 10.2174/0929867320666131119125045

Price: $65


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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