Method of identifying inhibitors of tie-2

C - Chemistry – Metallurgy – 07 – K

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C07K 14/71 (2006.01) A61P 35/00 (2006.01) G01N 33/68 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2404532

The present invention relates to polypeptides which comprise the ligand binding domain of Tie-2, crystalline forms of these polypeptides and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Tie-2. The invention also relates to the use of the three dimensional structure of the Tie-2 catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential inhibitors of Tie-2 activity, for example, compounds which inhibit the binding of a native substrate to the Tie-2 catalytic domain.

La présente invention concerne des polypeptides contenant le domaine de liaison du ligand de Tie-2, les formes cristallines de ces polypeptides ainsi que l'utilisation de ces formes cristallines pour déterminer la structure tridimensionnelle du domaine catalytique de Tie-2. En outre, cette invention concerne l'utilisation de cette structure tridimensionnelle du domaine catalytique de Tie-2, à la fois seule ou associée à des inhibiteurs, dans des procédés de désignation et/ou d'identification des inhibiteurs potentiels de l'activité de Tie-2, par exemple, des composés qui inhibent la liaison d'un substrat natif au domaine catalytique de Tie-2.

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