Selection of allosteric regulators with class iii g...

G - Physics – 01 – N

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Details

G01N 33/566 (2006.01) C12N 15/00 (2006.01) G01N 33/15 (2006.01) C07K 14/705 (2006.01) C12Q 1/68 (2006.01)

Patent

CA 2526695

The invention relates to a method for identifying and selecting a compound acting as an allosteric regulator of a GPCR-III. According to said method, the activity level of a recombinant GPCR-III (GPCR-III-?), essentially depleted of the extracellular domain of the corresponding native GPCR-III, in the presence of a given compound, is compared to the activity level of the same GPCR-III-? in the absence of said compound, enabling positive or negative allosteric regulators of GPCRs-III to be identified and selected. The invention also relates to the application of one such method for identifying and selecting compounds of interest in fields of activity such as pharmacy, the agro-food industry, the environment, ecology and basic research.

La présente invention concerne un procédé d'identification et sélection d'un composé agissant comme régulateur allostérique d'un RCPG-III. Selon ce procédé, le niveau d'activité d'un RCPG-III recombinant (RCPG-III-.DELTA.), essentiellement dépourvu du domaine extracellulaire du RCPG-III natif correspondant, en présence d'un composé donné, est comparé à celui du même RCPG-III-.DELTA., en l'absence dudit composé. Ce procédé permet ainsi d'identifier et sélectionner des régulateurs allostériques positifs ou négatifs des RCPG-III. L'invention vise en outre l'application d'un tel procédé à l'identification et la sélection de composés d'intérêt dans des domaines d'activités tels que la pharmacie, l'industrie agro-alimentaire, l'environnement, l'écologie et la recherche fondamentale.

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