Conjugates of proteins and bifunctional ligands

C - Chemistry – Metallurgy – 07 – K

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C07K 16/30 (2006.01) A61K 47/48 (2006.01) A61K 51/10 (2006.01)

Patent

CA 2158054

Provided are conjugates useful in cancer, cardiovascular or infectious disease detection and/or therapy. The conjugate is of a ligand and protein. The ligand has a moiety capable of binding to mercapto groups and is capable of chelating a metal useful for detection or therapy. The protein reacts with a substance associated with a targeted cell, pathologic lesion or pathogen. The protein prior to conjugation has at least one mercapto group which becomes a site for conjugation to the ligand. Also provided are metal chelates of the conjugate, methods of detection and therapy, methods for producing the conjugate and pharmaceutical compositions of the conjugates.

L'invention concerne des conjugués utiles pour la détection et/ou la thérapie du cancer, des maladies cardio-vasculaires ou infectieuses. Le conjugué se compose d'un ligand et d'une protéine. Le ligand possède une fraction qui peut se lier aux groupes mercapto et qui peut susciter la chélation d'un métal utile à la détection ou à la thérapie. La protéine réagit avec une substance associée à une cellule-cible, une lésion pathologique ou un pathogène. Avant conjugaison, la protéine comporte au moins un groupe mercapto qui devient le site de conjugaison avec le ligand. L'invention concerne également des chélates métalliques du conjugué, des procédés de détection et des protocoles thérapeutiques, des procédés de production du conjugué et des compositions pharmaceutiques des conjugués.

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