Conjugated peptide nucleic acids having enhanced cellular...

C - Chemistry – Metallurgy – 07 – K

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C07K 2/00 (2006.01) A61K 9/127 (2006.01) A61K 31/70 (2006.01) A61K 38/00 (2006.01) A61K 47/48 (2006.01) C07H 21/00 (2006.01) C07K 14/00 (2006.01) C08G 69/48 (2006.01)

Patent

CA 2291839

Peptide nucleic acids conjugated to lipophilic groups and incorporated into liposomes exhibit enhanced cellular uptake and distribution. Cellular uptake and distribution of peptide nucleic acids also increases with the introduction of an amino acid side chain into the backbone of peptide nucleic acids. Methods of modulating cellular uptake and methods for treating animals are provided. The peptide nucleic acids of the invention comprise naturally- occurring nucleobases and non-naturally-occurring nucleobases attached to a polyamide backbone.

L'invention concerne des acides nucléiques peptidiques conjugués à des groupes lipophiles, et incorporés dans des liposomes, qui présentent une fixation et une distribution cellulaire accrues. La fixation et la distribution cellulaire d'acides nucléiques s'accroît également avec l'introduction d'une chaîne latérale d'acides aminés dans le squelette des acides nucléiques peptidiques. L'invention concerne des procédés permettant de moduler la fixation cellulaire, et des procédés permettant de traiter des animaux. Les acides nucléiques peptidiques de l'invention comportent des bases naturelles, et des bases non naturelles fixées à un squelette de polyamide.

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