C - Chemistry – Metallurgy – 12 – N
Patent
C - Chemistry, Metallurgy
12
N
C12N 15/18 (2006.01) C07K 14/705 (2006.01) C07K 14/71 (2006.01) C30B 29/58 (2006.01) G01N 23/20 (2006.01) G01N 33/567 (2006.01)
Patent
CA 2340598
A 2.4 .ANG. crystal structure of a protein construct containing the catalytic kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2/KDR), a key enzyme in angiogenesis, has been determined in an unliganded, phosphorylated state. This protein construct, contains a modified catalytic linker and has comparable in vitro kinase activity to constructs containing the entire KID. The resulting construct retains comparable in vitro kinase activity to that of the wild-type KID, and more importantly, allows complete crystallization of the protein such that it may be characterized by X-ray crystallography. The present invention further discloses the use of x-ray crystallographic data for identification and construction of possible therapeutic compounds in the treatment of various disease conditions.
On a identifié une structure cristalline de 2,4 .ANG. d'une construction protéique contenant le domaine catalytique de la kinase, du récepteur 2 du facteur de croissance de l'endothélium vasculaire (VEGFR2/KDR), une enzyme clé dans l'angiogénèse, à l'état phosphorylé et non ligand. Cette construction protéique contient un segment de liaison catalytique et possède une activité de kinase in vitro comparable aux constructions contenant le domaine d'insertion de la kinase (KID). La construction résultante conserve une activité de kinase in vitro comparable à celle du KID du type sauvage, et mieux encore, permet la cristallisation complète de la protéine de sorte qu'elle puisse être caractérisée par cristallographie par rayons X. L'invention porte encore sur l'utilisation de données de cristallographie par rayons X, pour l'identification et la construction d'éventuels composés thérapeutiques dans le traitement de divers états pathologiques.
Appelt Krzysztof
Gehring Michael R.
Kan Chen-Chen
Mctigue Michele A.
Mroczkowski Barbara
Agouron Pharmaceuticals Inc.
Smart & Biggar
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