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METHOD TO IDENTIFY LIGANDS FOR SIGMA-1 RECEPTORS

机译:识别SIGMA-1受体配体的方法

摘要

An assay for identifying ligands of the σι receptor based on a fusion protein comprising the σι receptor flanked by two fluorophores, so that said fluorophores are capable of producing constitutive FRET when no ligand is bound to the σι receptor. The fusion protein of the invention also allows the simultaneous determination whether the newly determined ligand is an agonist or an antagonist. Said fusion protein has been expressed in a cell, giving rise to a new cellular model useful for identifying σι receptor ligands, and additionally for discriminating between agonists and antagonists.
机译:基于包含侧翼为两个荧光团的σ1受体的融合蛋白的σ1受体的配体的鉴定的测定法,使得当没有配体与σ1受体结合时,所述荧光团能够产生组成型FRET。本发明的融合蛋白还允许同时确定新确定的配体是激动剂还是拮抗剂。所述融合蛋白已在细胞中表达,产生了新的细胞模型,可用于鉴定σ1受体配体,另外还可用于区分激动剂和拮抗剂。

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