Determination of the 3d-structure of an extracellular domain...

C - Chemistry – Metallurgy – 07 – K

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C07K 14/72 (2006.01) G01N 33/50 (2006.01)

Patent

CA 2576435

The present invention relates to a method for identifying modulators of B1 G- protein coupled receptors. The present invention also relates to a method for identifying an antagonist or agonist of the corticotropin-releasing factor receptor 2 (CRFR2). The present invention also relates to a method for improving antagonists or agonists of CRFR2. The present invention also relates to the three-dimensional structure of CRFR2 as representative of the B1 GPCR subfamily and its use as a basis for rational drug design of antagonist or agonists of B1 GPCRs.

L'invention concerne un procédé permettant d'identifier des modulateurs de récepteurs couplés à la protéine G B1. L'invention concerne également un procédé permettant d'identifier un antagoniste ou un agoniste du récepteur 2 du facteur de libération de la corticotropine (CRFR2). L'invention concerne également un procédé permettant d'améliorer les antagonistes ou les agonistes du CRFR2. L'invention concerne en outre une structure tridimensionnelle du CRFR2 telle que représentant la sous-famille du B1 GPCR et son utilisation en tant que base pour l'élaboration rationnelle de médicaments de type antagonistes ou agonistes des B1 GPCR.

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