POLYIMIDAZOLE CONJUGATED OLIGONUCLEOTIDES REACH THE NUCLEUS OF HELA CELLS

Abstract

Oligonucleotide models bearing 6, 12 or 18 histamine residues were synthesized on solid support and labeled with fluorescein. Only the oligo with 6 histamine residues showed a high uptake in HeLa cells with a nuclear localization. Experiment a 4°C or with bafilomicyn A₁ suggest that uptake proceeded by an endocytosis mechanism followed by a destabilization of the membrane. Once in the cytoplasm the oligo reached rapidly the nucleus.

ACKNOWLEDGMENTS

This work was supported by grants from “Association pour la Recherche contre le Cancer” (ARC) and the “Comités de l'Aude et des Pyrénées Orientales de la Ligue contre le Cancer”.