Bioluminescence Resonance Energy Transfer Based G Protein-Activation Assay to Probe Duration of Antagonism at the Histamine H<sub>3</sub> Receptor

Bioluminescence Resonance Energy Transfer Based G Protein-Activation Assay to Probe Duration of Antagonism at the Histamine H<sub>3</sub> Receptor

Duration of receptor antagonism, measured as the recovery of agonist responsiveness, is gaining attention as a method to evaluate the &#8216;effective&#8217; target-residence for antagonists. These functional assays might be a good alternative for kinetic binding assays in competition with r...

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Bibliographic Details
Main Authors: Tamara A. M. Mocking, Maurice C. M. L. Buzink, Rob Leurs, Henry F. Vischer
Format: Article
Language:English
Published: MDPI AG 2019-07-01
Series:International Journal of Molecular Sciences
Subjects:
histamine H<sub>3</sub> receptor (H<sub>3</sub>R)
G protein-coupled receptor (GPCR)
re-equilibration
ligand binding kinetics
residence time
Online Access:https://www.mdpi.com/1422-0067/20/15/3724

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https://www.mdpi.com/1422-0067/20/15/3724

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