Asparaginyl hydroxylases and modulators thereof

C - Chemistry – Metallurgy – 12 – Q

Patent

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C12Q 1/26 (2006.01) C12Q 1/00 (2006.01) G01N 33/573 (2006.01)

Patent

CA 2502541

A method of identifying, screening, characterising or designing a chemical entity, which mimics or binds to FIH, is described. The method comprises comparing a structural model of FIH with a structural model for said chemical entity, wherein said structural model of FIH is derived from structural factors or structural coordinates determined by subjecting to X-ray diffraction measurements a crystal comprising FIH. Such chemical entities may be used in the treatment of a condition associated with increased or decreased HIF levels or activity.

L'invention concerne un procédé d'identification, de criblage, de caractérisation ou de conception d'une entité chimique qui imite ou se lie au FIH. Ledit procédé comprend la comparaison entre un modèle structurel de FIH et un modèle structurel de ladite entité chimique, dans laquelle le modèle structurel de FIH est dérivé des facteurs structurels ou des coordonnées structurelles déterminés lorsqu'un cristal comprenant du FIH est soumis à des mesures de diffraction des rayons X. Lesdites entités chimiques peuvent être utilisées dans le traitement d'un état pathologique associé aux taux et à l'activité croissants ou décroissant de HIF.

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