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 acting as an allosteric regulator of a GPCR-III. According to this method, the level of activity of a recombinant RCPG-III (RCPG-III-DELTA.), Essentially devoid of the corresponding native RCPG-III extracellular domain, in the presence of a given compound, is compared with that the same RCPG-III-.DELTA., in the absence of said compound. This method thus makes it possible to identify and select positive or negative allosteric regulators of GPCR-IIIs. The invention also aims to apply such a method to the identification and selection of compounds of interest in fields of activity such as pharmacy, the food industry, the environment, the ecology and basic research.
机译:本发明涉及鉴定和选择作为GPCR-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上没有相应天然RCPG-III胞外域的重组RCPG-III(RCPG-III-DELTA)的活性水平与相同化合物进行比较。在没有所述化合物的情况下为RCPG-III-Δ。因此,该方法使得可以鉴定和选择GPCR-III的正或负变构调节剂。本发明的目的还在于将这种方法应用于在诸如制药,食品工业,环境,生态学和基础研究等活动领域中感兴趣的化合物的鉴定和选择。

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