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.…
Laura H. Heitman
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…
Structural basis of selective cannabinoid CB2 receptor activation
Abstract Cannabinoid CB2 receptor (CB2R) agonists are investigated as therapeutic agents in the clinic. However, their molecular mode-of-action is not…
Development of a Cannabinoid-Based Photoaffinity Probe to Determine the Δ8/9-Tetrahydrocannabinol Protein Interaction Landscape in Neuroblastoma Cells
Abstract Introduction: Δ9-Tetrahydrocannabinol (THC), the principle psychoactive ingredient in Cannabis, is widely used for its therapeutic effects in a large…
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.…