首页> 外国专利> 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

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

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.
机译:本发明涉及鉴定和选择用作RCPG-III的变构调节剂的化合物的方法。根据该方法,将在给定化合物存在下基本不含相应天然RCPG-III胞外域的重组RCPG-III(RCPG-III-Δ)的活性水平与该活性进行了比较。在不存在所述化合物的情况下,具有相同的RCPG-III-Δ。因此,该过程使得可以鉴定和选择RCPG-III的正或负变构调节剂。本发明还涉及这种方法在诸如制药,食品工业,环境,生态学和基础研究等活性领域中鉴定和选择感兴趣的化合物的应用。

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