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Method for identifying ligands for sigma-1 receptors

机译:识别sigma-1受体配体的方法

摘要

A fusion protein comprising (i) a receiver σ1 or a functionally equivalent variant thereof, wherein said functional equivalent σ1 receptor has an identity amino acid sequence of at least 70% with the human receptor σ1 wildtype and wherein said functional equivalent of σ1 receptor has the ability to bind to haloperidol with an affinity of at least 10% of the human σ1 wild type receptor, (ii) a residue of donor fluorescent protein, and (iii) a residue of fluorescent protein acceptor, wherein said residues fluorescent protein donor and acceptor are capable of producing energy transfer fluorescence resonance (FRET) and wherein the σ1 receptor is flanked by other donor fluorescent protein and other fluorescent acceptor protein.
机译:包含(i)受体σ1或其功能等效变体的融合蛋白,其中所述功能等效σ1受体与人受体σ1野生型具有至少70%的同一性氨基酸序列,并且其中所述σ1受体功能等同物具有以至少10%的人σ1野生型受体亲和力与氟哌啶醇结合的能力,(ii)供体荧光蛋白的残基,和(iii)荧光蛋白受体的残基,其中所述残基为荧光蛋白供体和受体能够产生能量转移荧光共振(FRET),并且其中σ1受体侧翼于其他供体荧光蛋白和其他荧光受体蛋白。

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