Multiple intramolecular triggers converge to preferential G protein coupling in the CB2R
Abstract G protein-coupled receptors (GPCRs) are important therapeutic drug targets for a wide range of diseases. Upon activation, GPCRs can…
Abstract G protein-coupled receptors (GPCRs) are important therapeutic drug targets for a wide range of diseases. Upon activation, GPCRs can…
Abstract Introduction: The kinetics of ligand binding to G protein-coupled receptors (GPCRs) is an important optimization parameter in drug discovery.…
Abstract We report a blueprint for the rational design of G protein coupled receptor (GPCR) ligands with a tailored functional…
Abstract Monoacylglycerol lipase (MAGL) regulates endocannabinoid 2-arachidonoylglycerol (2-AG) and eicosanoid signalling. MAGL inhibition provides therapeutic opportunities but clinical potential is…
Abstract Chemical tools and methods that report on G protein-coupled receptor (GPCR) expression levels and receptor occupancy by small molecules…
Abstract The cannabinoid CB2 receptor (CB2R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases.…