Optical techniques to analyze real-time activation and signaling of G-protein-coupled receptors

摘要: The activation of G-protein-coupled receptors (GPCRs) is traditionally measured either by monitoring downstream physiological events or membrane-based biochemical assays. Neither these approaches permits detailed kinetic spatial analysis receptor and signaling. Recently, several optical techniques have been developed to monitor using purified reconstituted GPCRs observing GPCRs, G proteins second messengers in intact cells. These are providing, literally, new views on both the mechanistic basis signaling process properties GPCR-mediated signals. They suggest that agonists can activate within milliseconds, different compounds induce distinct active conformations G-protein rate-limiting step GPCR signaling, cellular signals be temporally spatially confined. also raising controversial issues, such as whether not pre-coupled dissociate during activation.