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Current Topics in Medicinal Chemistry


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

Chemical Modifications to Improve the Cellular Uptake of Oligonucleotides

Author(s): Francoise Debart, Said Abes, Gaelle Deglane, Hong M. Moulton, Philippe Clair, Michael J. Gait, Jean-Jacques Vasseur and Bernard Lebleu

Volume 7, Issue 7, 2007

Page: [727 - 737] Pages: 11

DOI: 10.2174/156802607780487704

Price: $65


Specific control of gene expression by synthetic oligonucleotides (ON) is now widely used for target validation but clinical applications are limited by ON bioavailability. Moreover, most currently used strategies for physical and chemical delivery cannot be easily implemented in vivo. This article reviews new strategies which appear promising for ON delivery. The first part deals with ON chemical modifications aiming at improving cellular uptake as for instance the grafting of cationic groups on the ON backbone. The second part concerns ON conjugation to cell penetrating peptides.

Keywords: cationic lipids, siRNA, spermidine, guanidine-based PNA, Cell Penetrating Peptides

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