A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand binding assay.
L. Borrega-Roman, B. L. Hoare, M. Kosar, R. C. Sarott, K. J. Patej, J. Bouma, M. Scott-Dennis, E. J. Koers, T. Gazzi, L. Mach, S. Barrondo, J. Salles, W. Guba, E. Kusznir, M. Nazare, , D. B. Veprintsev
This paper develops a TR-FRET-based assay to measure ligand binding kinetics for CB1R and CB2R, finding that D77 enables accurate determination of on- and off-rates for various agonists and antagonists.
bioRxiv · Jul 16, 2024Pharmacology & Toxicology