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Pichon, C ; Roufai, MB ; Monsigny, M ; Midoux, P

Histidylated oligolysines increase the transmembrane passage and the biological activity of antisense oligonucleotides

Nucleic Acids Research 28 (2) 504-512

par Administrateur - publié le , mis à jour le

Abstract :

We have designed histidylated oligolysines which increase the uptake, the cytosolic delivery and the nuclear accumulation of antisense oligonucleotides (ODN), Flow cytometry analysis showed a 10-fold enhancement of the ODN uptake in the presence of histidylated oligolysines. The intracellular localizations of fluorescein-labeled ODN and of rhodamine-labeled histidylated oligolysines were investigated by confocal microscopy. Histidylated oligolysines favor the cytosolic delivery of ODN from endosomes and increase their nuclear accumulation.