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 Chemjournal_title
Current medicinal chemistryauthors
Wang CF,Auriola S,Hirvonen J,Santos HAdoi
10.2174/0929867320666131119125045subject
Has Abstractpub_date
2014-04-01 00:00:00pages
1247-54issue
10eissn
0929-8673issn
1875-533Xpii
CMC-EPUB-57517journal_volume
21pub_type
杂志文章abstract::The synthesis and biological evaluation of carbohydrate mimetics has begun to more clearly define the diverse roles of carbohydrates in nature. Often the strategy invoves the design and synthesis of glycosyltransferase and glycosidase inhibitors both as tools to elucidate the mechanism of action of these enzymes and a...
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