Tissue specific peptide conjugates and methods

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 7/02 (2006.01) A61K 47/48 (2006.01) C07H 21/00 (2006.01) C07K 5/033 (2006.01) C12N 15/113 (2010.01) C12N 15/87 (2006.01)

Patent

CA 2691673

Cell-penetrating peptides useful for targeting a therapeutic compound to a selected mammalian tissue, methods for their identification, methods of forming conjugate compounds containing such peptides, and conjugates formed thereby are dis-closed. The cell-penetrating peptides are 8 to 30 amino acid residues in length and consist of subsequences selected from the group consisting of RXR, RX, RB, and RBR; where R is arginine, B is .beta.-alanine, and each X is independently -C(O)-(CHR1)n-NH-, where n is 4-6 and each R1 is independently H or methyl, such that at most two R1's are methyl. In one embodiment, X is a 6-aminohexanoic acid residue.

La présente invention concerne des peptides pénétrant les cellules utiles pour diriger de façon ciblée un composé thérapeutique sur un tissu de mammifère choisi, des procédés pour leur identification, des procédés permettant de former des composés conjugués contenant de tels peptides, et des conjugués formés de ce fait. Les peptides pénétrant les cellules sont des résidus ayant une longueur de 8 à 30 acides aminés et sont composés de sous-séquences choisies dans le groupe constitué par RXR, RX, RB, et RBR; où R est de l'arginine, B est de la ß-alanine, et chaque X est indépendamment -C(O)-(CHR1 )n-NH-, où n vaut 4 à 6 et chaque R1 est indépendamment H ou un groupe méthyle, de telle sorte que deux R1 maximum soient des groupes méthyle. Dans un mode de réalisation, X est un résidu d'acide 6-aminohexanoïque.

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