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…
David A. Sykes
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.…
Structural basis of THC analog activity at the Cannabinoid 1 receptor
Abstract Tetrahydrocannabinol (THC) is the principal psychoactive compound derived from the cannabis plant Cannabis sativa and approved for emetic conditions,…
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…