Improved conjugates

C - Chemistry – Metallurgy – 12 – N

Patent

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Details

C12N 15/62 (2006.01) A61K 45/06 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01) A61P 35/00 (2006.01) C07K 14/21 (2006.01) C07K 14/34 (2006.01) C07K 14/38 (2006.01) C07K 14/415 (2006.01) C07K 16/00 (2006.01) C07K 19/00 (2006.01) C12N 15/63 (2006.01)

Patent

CA 2668017

Novel conjugates are disclosed which comprise (a) a ligand that binds to a surface molecule on a target cell, such as a cancer cell; (b) an effector molecule that is to be delivered into the cell, such as a toxin; and (c) a linker sequence that couples the ligand and the effector molecule wherein the linker comprises at least one protease cleavage site corresponding to a protease found in the intracellular trafficking pathway of the effector molecule; wherein the cleavage of the linker by the protease uncouples the effector molecule from the ligand.

La présente invention concerne de nouveaux conjugués qui comprennent (a) un ligand qui se lie à une molécule de surface sur une cellule cible, telle qu'une cellule cancéreuse ; (b) une molécule effectrice qui doit être délivrée à l'intérieur de la cellule, telle qu'une toxine ; et (c) une séquence de liaison qui relie le ligand et la molécule effectrice dans laquelle le lieur comprend au moins un site de clivage par protéase correspondant à une protéase se trouvant dans la voie d'acheminement intracellulaire de la molécule effectrice ; ledit clivage du lieur par la protéase décrochant la molécule effectrice du ligand.

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