Homogeneous, Real-Time NanoBRET Binding Assays for the Histamine H3 and H4 Receptors on Living Cells
作者： Tamara A. M. Mocking , Eléonore W. E. Verweij , Henry F. Vischer , Rob Leurs
关键词:
摘要: Receptor-binding affinity and ligand-receptor residence time are key parameters for the selection of drug candidates routinely determined using radioligand competition-binding assays. Recently, a novel bioluminescence resonance energy transfer (BRET) method utilizing NanoLuc-fused receptor was introduced to detect fluorescent ligand binding. Moreover, this NanoBRET gives opportunity follow binding on intact cells in real time, therefore, results might better reflect vivo conditions as compared with used cell homogenates or purified membrane fractions. In study, real-time NanoBRET-based assay established validated unlabeled ligands histamine H3 (H3R) H4 cells. Obtained times clinically tested H3R antagonists were reflected by their duration antagonism functional recovery assay.
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