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Issue 4, 2013
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Facile solid-phase synthesis of a highly stable poly(ethylene glycol)–oligonucleotide conjugate

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Abstract

A novel solid-phase synthesis method for poly(ethylene glycol) (PEG)–oligonucleotide conjugates was developed to increase the stability of therapeutic oligonucleotides such as antisense oligonucleotides and siRNA. A prepared solid phase was pre-installed with PEG to provide oligonucleotides modified with PEG at the 3′ terminus. Compared with the conventional liquid-phase synthesis method, the developed solid-phase method is simple and reproducible. PEGylation at the 3′ terminus was confirmed to stabilize not only DNA but also RNA more than PEGylation at the 5′ terminus, which has been widely used so far.

Graphical abstract: Facile solid-phase synthesis of a highly stable poly(ethylene glycol)–oligonucleotide conjugate

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Publication details

The article was received on 28 Aug 2012, accepted on 08 Nov 2012 and first published on 09 Nov 2012


Article type: Paper
DOI: 10.1039/C2TB00031H
J. Mater. Chem. B, 2013,1, 529-535

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    Facile solid-phase synthesis of a highly stable poly(ethylene glycol)–oligonucleotide conjugate

    Y. Ikeda, H. Kawasaki, S. Ichinohe and Y. Nagasaki, J. Mater. Chem. B, 2013, 1, 529
    DOI: 10.1039/C2TB00031H

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