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SELECTION OF ALLOSTERIC REGULATORS WITH CLASS III G PROTEIN-COUPLED RECEPTORS DEPLETED OF THE EXTRACELLULAR DOMAIN
SELECTION OF ALLOSTERIC REGULATORS WITH CLASS III G PROTEIN-COUPLED RECEPTORS DEPLETED OF THE EXTRACELLULAR DOMAIN
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机译:选择III型G蛋白偶联受体的胞外域缺失的变构调节剂
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摘要
The present invention relates to a method for identifying and selecting a compound which acts as an allosteric regulator of an RCPG-III. According to this method, the activity level of a recombinant RCPG-III (RCPG-III-.DELTA.), Essentially devoid of the extracellular domain of the corresponding native RCPG-III, in the presence of a given compound, is compared to that of the same RCPG-III-.DELTA., in the absence of said compound. This process thus makes it possible to identify and select positive or negative allosteric regulators of RCPG-III. The invention further relates to the application of such a method to the identification and selection of compounds of interest in fields of activity such as pharmacy, the food industry, the environment, ecology and basic research.
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