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• W2892830761 abstract "Receptor-binding affinity and ligand-receptor residence time are key parameters for the selection of drug candidates and are routinely determined using radioligand competition-binding assays. Recently, a novel bioluminescence resonance energy transfer (BRET) method utilizing a NanoLuc-fused receptor was introduced to detect fluorescent ligand binding. Moreover, this NanoBRET method gives the opportunity to follow fluorescent ligand binding on intact cells in real time, and therefore, results might better reflect in vivo conditions as compared with the routinely used cell homogenates or purified membrane fractions. In this study, a real-time NanoBRET-based binding assay was established and validated to detect binding of unlabeled ligands to the histamine H₃ receptor (H₃R) and histamine H₄ receptor on intact cells. Obtained residence times of clinically tested H₃R antagonists were reflected by their duration of H₃R antagonism in a functional receptor recovery assay." @default.
• W2892830761 created "2018-10-05" @default.
• W2892830761 creator A5046505895 @default.
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• W2892830761 date "2018-09-24" @default.
• W2892830761 modified "2023-10-18" @default.
• W2892830761 title "Homogeneous, Real-Time NanoBRET Binding Assays for the Histamine H₃ and H₄ Receptors on Living Cells" @default.
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• W2892830761 doi "https://doi.org/10.1124/mol.118.113373" @default.
• W2892830761 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30249614" @default.
• W2892830761 hasPublicationYear "2018" @default.
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