Methods of promoting uptake and nuclear accumulation of...

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A61K 31/785 (2006.01) A61K 45/06 (2006.01) C12N 15/63 (2006.01)

Patent

CA 2465886

A method for enhancing cellular uptake and redistributing gene regulating polyamides from the extranuclear areas in eukaryotic cells to the nucleus thereof. The method consists of administering to the eukaryotic cells a molecular trafficking compound. The administered molecular trafficking compound affects cellular pathways and mechanisms that accumulate polyamides in cytoplasmic vessicles and/or efflux polyamides from the intracellular regions of cell. The method also includes modifying polyamides to contain negatively-charged or acidic moieties wherein the moieties inhibit the accumulation of polyamides in cellular lysosomes. By affecting the cellular pathways and mechanisms, the polyamides are redistributed throughout the cell, whereby nuclear accumulation of the polyamides is enhanced.

Procédé servant à augmenter l'absorption cellulaire et à redistribuer des polyamides de régulation génique depuis les zones extranucléaires de cellules eucaryotes jusqu'au noyau de ces cellules. Ce procédé consiste à administrer à ces cellules eucaryotes un composé de trafic moléculaire. L'administration de ce composé exerce un effet sur les trajets et les mécanismes cellulaires accumulant des polyamides dans des vésicules cytoplasmiques et/ou évacuant ces polyamides hors des zones intracellulaires de la cellule. Ce procédé consiste également à modifier les polyamides afin qu'ils contiennent des fractions à charge négative ou des fractions acides, ces fractions inhibant l'accumulation des polyamides dans les lysosomes cellulaires. L'effet exercé sur les trajets et les mécanismes cellulaires permet de redistribuer les polyamides au travers de la cellule et, par conséquent, d'augmenter l'accumulation nucléaire de ces polyamides.

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