Conjugation of peptides to antisense interleukin-6 via click chemistry.

Abstract:

: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.

journal_name

Curr Med Chem

authors

Wang CF,Auriola S,Hirvonen J,Santos HA

doi

10.2174/0929867320666131119125045

subject

Has Abstract

pub_date

2014-04-01 00:00:00

pages

1247-54

issue

10

eissn

0929-8673

issn

1875-533X

pii

CMC-EPUB-57517

journal_volume

21

pub_type

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