Chemical Modifications to Improve the Cellular Uptake of Oligonucleotides

Francoise      Debart; Said      Abes; Gaelle      Deglane; Hong   M.   Moulton; Philippe      Clair; Michael   J.   Gait; Jean-Jacques      Vasseur; Bernard      Lebleu

doi:10.2174/156802607780487704

Abstract

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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Current Topics in Medicinal Chemistry

Title: Chemical Modifications to Improve the Cellular Uptake of Oligonucleotides

Volume: 7 Issue: 7

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

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

Abstract: 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.

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Debart Francoise, Abes Said, Deglane Gaelle, Moulton M. Hong, Clair Philippe, Gait J. Michael, Vasseur Jean-Jacques and Lebleu Bernard, Chemical Modifications to Improve the Cellular Uptake of Oligonucleotides, Current Topics in Medicinal Chemistry 2007; 7 (7) . https://dx.doi.org/10.2174/156802607780487704