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
Current Topics in Medicinal Chemistry
Title: RNA Interference with Chemically Modified siRNA
Volume: 6 Issue: 9
Author(s): Hong-Yan Zhang, Quan Du, Claes Wahlestedt and Zicai Liang
Affiliation:
Keywords: terminal modifications, RNA sugar ring, lactosylated-PEG-siRNA conjugates, oligonucleotides, Backbone modifications
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.
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Cite this article as:
Zhang Hong-Yan, Du Quan, Wahlestedt Claes and Liang Zicai, RNA Interference with Chemically Modified siRNA, Current Topics in Medicinal Chemistry 2006; 6 (9) . https://dx.doi.org/10.2174/156802606777303676
DOI https://dx.doi.org/10.2174/156802606777303676 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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