Inhibitors of binding between proteins and macromolecular...

Details Inhibitors of binding between proteins and macromolecular... Inhibitors of binding between proteins and macromolecular...

G - Physics

01

N

G01N 33/53 (2006.01) C07K 14/52 (2006.01) C07K 14/715 (2006.01) G01N 33/50 (2006.01) G01N 33/543 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2383559

Disclosed is a compound which inhibits binding between a target protein and a macromolecular ligand of the target protein. The compound comprises a targeting group, an attaching group and, optionally a linker group. In one aspect of the invention, the targeting group is a moiety that binds non- covalently to a surface of the target protein with a Kd of greater than about 0.1 µM and within sufficient proximity to the target protein/macromolecular ligand binding site to inhibit binding between the target protein and the macromolecular ligand. In another aspect of the invention, targeting group is degradable in vivo. In yet another aspect of the invention, the compound comprises a linker group that is cleavable in vivo.

L'invention concerne un composé inhibant la liaison entre une protéine ciblée et un ligand macromoléculaire de cette protéine. Ce composé contient un groupe de ciblage, un groupe de fixation et, éventuellement, un groupe de liaison. Dans un aspect de l'invention, le groupe de ciblage est une fraction se liant de façon non covalente à une surface de la protéine ciblée avec un Kd supérieur à 0,1 µM et à proximité suffisante du site de liaison de la protéine ciblée et du ligand macromoléculaire pour inhiber la liaison entre ces derniers. Dans un autre aspect de l'invention, le groupe de ciblage est dégradable in vivo. Dans encore un autre aspect de l'invention, ce composé comprend un groupe de liaison pouvant se diviser in vivo.

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