Crystalline form of activated trap and use thereof for...

C - Chemistry – Metallurgy – 12 – N

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C12N 9/16 (2006.01)

Patent

CA 2355830

The invention relates to crystalline form of active TRAP (tartrate-resistant and purple acid phosphatases), preferably human or rat TRAP. The atomic structural coordinates are given as well as the conserved surface which is created by special atoms, relevant for the design of modulators or inhibitors of the human TRAP. This crystalline form of active TRAP can be used for structure-based drug design for specific modulator, activator or inhibitor of TRAP activity, useful in the treatment of diseases or degenerative conditions resulting in increased bone resorption, such as tissue damages, bone metabolic disorders, osteoporosis.

La présente invention concerne la forme cristalline du phosphatases TRAP actives (tartrate-resistant and purple acid phosphatases), de préférence les TRAP humaines ou murines. L'invention concerne également les coordonnées structurelles atomiques ainsi que la surface conservée qui est créée par des atomes spéciaux dans le cadre de la conception de modulateurs ou d'inhibiteurs de la TRAP humaine. Cette forme cristalline de la TRAP active convient pour la conception structurale de médicaments destinés à des modulateurs, des activateurs ou des inhibiteurs spécifiques de l'activité TRAP, lesquels modulateurs, activateurs et inhibiteurs spécifiques conviennent particulièrement au traitement d'affections ou d'états dégénératifs aboutissant à un accroissement de la résorption osseuse, tels que les dégâts tissulaires, les troubles du métabolisme osseux, et l'ostéoporose.

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