Issue 4, 2013
From the journal:

Journal of Materials Chemistry B

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

Yutaka Ikeda,ac   Hiromichi Kawasaki,a   Satoshi Ichinohea  and  Yukio Nagasaki*abcd  

* Corresponding authors

a Graduate School of Pure and Applied Science, University of Tsukuba, Japan
E-mail: yukio@nagalabo.jp
Fax: +81-29-853-5749
Tel: +81-29-853-5749

b International Center for Materials Nanoarchitectonics Satellite (WPI-MANA), National Institute for Materials Science (NIMS), University of Tsukuba, Japan

c CREST, Japan Science and Technology Agency (JST), Japan

d Master's School of Medical Sciences, Graduate School of Comprehensive Human Science, University of Tsukuba, Tennoudai 1-1-1, Tsukuba, Ibaraki 305-8573, Japan

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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Article information

DOI
https://doi.org/10.1039/C2TB00031H
Article type
Paper
Submitted
28 Aug 2012
Accepted
08 Nov 2012
First published
09 Nov 2012

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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