Peptides whose uptake by cells is controllable

Details Peptides whose uptake by cells is controllable Peptides whose uptake by cells is controllable

C - Chemistry, Metallurgy

07

K

C07K 19/00 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01) A61K 51/08 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) A61B 5/055 (2006.01) G01T 1/164 (2006.01)

Patent

CA 2611468

A generic structure for the peptides of the present invention includes A ~ X ~ B - C, where C is a cargo moiety, the B portion includes basic amino acids, X is a cleavable linker sequence, and the A portion includes acidic amino acids. The intact structure is not significantly taken up by cells; however, upon extracellular cleavage of X, the B ~ C portion is taken up, delivering the cargo to targeted cells. Cargo may be, for example, a contrast agent for diagnostic imaging, a chemotherapeutic drug, or a radiation-sensitizer for therapy. X may be cleaved extracellularly or intracellularly. The molecules of the present inventnon may be linear, cyclic, branched, or have a mixed structure.

La présente invention a trait à des peptides dont la structure générique comporte A X B - C, où C est un groupe fonctionnel de charge, la portion B comporte des acides aminés basiques, X est une séquence de liaison clivable, et la portion A comporte des acides aminés acides. La structure intacte n'est pas absorbée de manière importante par des cellules; cependant, lors du clivage extracellulaire de X, la portion B C est absorbée, délivrant la charge vers des cellules ciblées. La charge peut être, par exemple, un agent de contraste pour l'imagerie diagnostique, un médicament chimiothérapeutique, ou un agent de sensibilisation au rayonnement pour la thérapie. X peut être soumis à un clivage extracellulaire ou intracellulaire. Les molécules de la présente invention peuvent être linéaires, cycliques, ramifiées, ou présenter une structure mixte.

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