A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand-binding assay

A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand-binding assay

IntroductionThe kinetics of ligand binding to G protein-coupled receptors (GPCRs) is an important optimization parameter in drug discovery. Traditional radioligand assays are labor-intensive, preventing their application at the early stages of drug discovery. Fluorescence-based assays offer several...

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Main Authors: Leire Borrega-Roman, Bradley L. Hoare, Miroslav Kosar, Roman C. Sarott, Kacper J. Patej, Jara Bouma, Morgan Scott-Dennis, Eline J. Koers, Thais Gazzi, Leonard Mach, Sergio Barrondo, Joan Sallés, Wolfgang Guba, Eric Kusznir, Marc Nazaré, Arne C. Rufer, Uwe Grether, Laura H. Heitman, Erick M. Carreira, David A. Sykes, Dmitry B. Veprintsev
Format: Article
Language:English
Published: Frontiers Media S.A. 2025-04-01
Series:Frontiers in Pharmacology
Subjects:
time-resolved Forster resonance energy transfer- based binding assay
fluorescent ligand
kinetic ligand binding assay
cannabinoid type 1
cannabinoid type 2
cannabinoid receptors
Online Access:https://www.frontiersin.org/articles/10.3389/fphar.2025.1469986/full
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https://www.frontiersin.org/articles/10.3389/fphar.2025.1469986/full

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