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CONSTITUTIVELY DESENSITIZED G PROTEIN-COUPLED RECEPTORS

机译:本构去糖的G蛋白偶联受体

摘要

The present invention relates to modified G-protein coupled receptors (GPCRs). The modified GPCRs of the present invention include GPCRs that have been modified to have altered DRY motifs such that the modified GPCRs are constitutively desensitized. As such, the modified GPCRs of the present invention preferably localize to endocytic vesicles or endosomes in an agonist-independent manner. The invention also relates to methods of screening compounds and sample solutions for GPCR activity using the modified GPCRs.
机译:本发明涉及修饰的G蛋白偶联受体(GPCR)。本发明的修饰的GPCR包括被修饰为具有改变的DRY基序的GPCR,使得修饰的GPCR被组成性脱敏。这样,本发明的修饰的GPCR优选地以激动剂非依赖性的方式定位于内吞小泡或内体。本发明还涉及使用修饰的GPCR针对GPCR活性筛选化合物和样品溶液的方法。

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