Delivery of antisense oligonucleotides using cholesterol-modified sense dendrimers and cationic lipids |
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Authors: | Chaltin Patrick Margineanu Anca Marchand Damien Van Aerschot Arthur Rozenski Jef De Schryver Frans Herrmann Andreas Müllen Klaus Juliano Rudolph Fisher Michael H Kang Hyunmin De Feyter Steven Herdewijn Piet |
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Affiliation: | Laboratory for Medicinal Chemistry, Rega Institute, Catholic University of Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium. |
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Abstract: | Cholesterol modified mono-, di-, and tetrameric oligonucleotides were synthesized and hybridized with antisense oligonucleotides to study their incorporation in cationic liposomes together with the influence of this dendrimeric delivery system on biological activity. Electrostatic interactions seem to play the most important role during complexation with cationic lipids. This oligonucleotide formulation gives a small but significant increase in the inhibition of P-glycoprotein expression in a cellular system. |
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