Conjugates of transporter peptides and nucleic acid analogs,...

C - Chemistry – Metallurgy – 12 – N

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C12N 15/87 (2006.01) A61K 47/48 (2006.01) C07K 14/435 (2006.01) C07K 14/575 (2006.01) C12N 15/11 (2006.01)

Patent

CA 2298067

Constructs of peptides and nucleic acid analogs conjugated together for transport across a lipid membrane and for delivery into interactive contact with intracellular polynucleotides are disclosed. Transport is effected through at least the exterior membrane of a cell, and most likely also through the walls of subcellular structures separated from the cytosol by lipid membranes, including the nucleus, mitochondria, ribosomes, etc. Peptide nucleic acid (PNA) analog sequences conjugated through a labile disulfide bond to transporting peptides, are intracellulary cleaved, and target mRNA (antigene) or dsDNA (antisense).

L'invention concerne des produits de synthèse de peptides et des analogues d'acides nucléiques conjugués pour traverser une membrane lipidique et pour être amenés en contact interactif avec des polynucléotides intracellulaires. Le transport se fait à travers au moins la membrane extérieure d'une cellule et, de manière plus vraisemblable, à travers les parois de structures infracellulaires séparées du cytosol par des membranes lipidiques, telles que le noyau, la mitochondrie, les ribosomes, etc. Les séquences d'analogues d'acides nucléiques peptidiques (PNA) conjuguées par un pont disulfure labile aux peptides transporteurs sont clivées à l'intérieur des cellules et ciblent l'ARN messager (antigène) ou l'ADN bicaténaire (antisens).

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