A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand binding assay.
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 A. Kusznir, Marc Nazaré, , Dmitry 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.
Frontiers in Pharmacology · Apr 9, 2025Peer-reviewedPharmacology & Toxicology