Site-specific labeling of disulfide-containing targeting...

Details Site-specific labeling of disulfide-containing targeting... Site-specific labeling of disulfide-containing targeting...

A - Human Necessities

61

K

A61K 47/48 (2006.01) A61K 51/08 (2006.01) A61K 51/10 (2006.01)

Patent

CA 2346170

A method of producing a diagnostic or therapeutic conjugate of a protein, polypeptide or peptide containing at least one disulfide bond which is necessary to maintain its biological activity, and bearing at least one thiol-containing moiety linked thereto through a hydrazone or hydrazine linkage, is effected by contacting said protein, polypeptide or peptide with a thiol-reactive diagnostic or therapeutic agent, either preformed or generated in situ, to form a stable diagnostic or therapeutic conjugate of the protein, polypeptide or peptide without substantial cleavage of the disulfide bond. Diagnostic and therapeutic conjugates produced using the foregoing method, as well as kits for carrying out the method are provided.

L'invention concerne un procédé relatif à la fabrication d'un conjugué diagnostique ou thérapeutique d'une protéine, d'un polypeptide ou d'un peptide contenant au moins une liaison disulfure nécessaire à l'activité biologique propre, et comportant au moins une fraction à base de thiol liée par une liaison hydrazone ou hydrazine. On met en contact la protéine, le polypeptide ou le peptide avec un agent diagnostique ou thérapeutique réagissant avec le thiol, soit de manière préformée soit en réalisation in situ, de manière à élaborer un conjugué diagnostique ou thérapeutique stable correspondant, sans clivage substantiel de la liaison disulfure. L'invention concerne également les conjugués résultants et des kits permettant de mettre en oeuvre le procédé.

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