C - Chemistry – Metallurgy – 12 – Q
Patent
C - Chemistry, Metallurgy
12
Q
C12Q 1/70 (2006.01) C12N 9/64 (2006.01) C12Q 1/68 (2006.01) G01N 33/48 (2006.01) G01N 33/50 (2006.01) G06F 19/00 (2006.01)
Patent
CA 2564584
The present invention includes crystallized HDM2 peptides as well as descriptions of the X-ray diffraction patterns of the crystals. The diffraction patterns allow the three dimensional structure of HDM2 to be determined at atomic resolution so that ligand binding sites on HDM2 can be identified and the interactions of ligands with HDM2 amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MDM2 and HDM2 oncoproteins.
La présente invention comporte des peptides cristallisés HDM2 de même que des descriptions des motifs de diffraction aux rayons X des cristaux. Les motifs de diffraction permettent de déterminer la structure tridimensionnelle de HDM2 avec une définition atomique de façon à pouvoir identifier les sites de liaison de ligand en HDM2 et modéliser les interactions des ligands avec les résidus d~acide aminé HDM2. Les modèles élaborés à l~aide de ces cartes permettent de concevoir des ligands susceptibles de remplir des fonctions d~agents actifs comme par exemple, mais sans s~y limiter, une fonction inhibitrice d~oncoprotéines MDM2 et HDM2.
Deckman Ingrid
Grasberger Bruce
Maguire Diane
Schubert Carsten
Spurlino John
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
Ortho-Mcneil Pharmaceutical Inc.
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