| Autor: |
Tamara A M, Mocking, Eléonore W E, Verweij, Henry F, Vischer, Rob, Leurs |
| Rok vydání: |
2018 |
| Předmět: |
|
| Zdroj: |
Molecular pharmacology. 94(6) |
| ISSN: |
1521-0111 |
| Popis: |
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 H |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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