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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

RNA Interference with Chemically Modified siRNA

Author(s): Hong-Yan Zhang, Quan Du, Claes Wahlestedt and Zicai Liang

Volume 6, Issue 9, 2006

Page: [893 - 900] Pages: 8

DOI: 10.2174/156802606777303676

Price: $65

Abstract

siRNA has become an indispensable tool for functional characterization of genes. It has also demonstrated tremendous potential as a new generation of drug candidates. Although the technology works very well to a great panel of cells in vitro, it is still a challenge to translate the success into in vivo target validation easiness and, even more difficult, into therapeutic applications. With a number of chemically modified compounds under initial clinical trial from several commercial entities, the interests in chemical modification of siRNA have become heightened. In this review we have tried to touch on most of the chemical modifications of RNA that have been tested in the siRNA landscape, but maintained a focus on the backbone modifications, and 2-modifications on the ribose ring. It is anticipated that more modifications and more systematic comparisons between different modifications will be performed to draw more educated conclusions over some of the modifications.

Keywords: terminal modifications, RNA sugar ring, lactosylated-PEG-siRNA conjugates, oligonucleotides, Backbone modifications


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