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…
Uwe Grether
A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand-binding assay
Abstract Introduction: The kinetics of ligand binding to G protein-coupled receptors (GPCRs) is an important optimization parameter in drug discovery.…
Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists
Abstract We report a blueprint for the rational design of G protein coupled receptor (GPCR) ligands with a tailored functional…
A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence
Abstract Monoacylglycerol lipase (MAGL) regulates endocannabinoid 2-arachidonoylglycerol (2-AG) and eicosanoid signalling. MAGL inhibition provides therapeutic opportunities but clinical potential is…
Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells
Abstract Chemical tools and methods that report on G protein-coupled receptor (GPCR) expression levels and receptor occupancy by small molecules…
Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity
Abstract The cannabinoid CB2 receptor (CB2R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases.…