The G-protein coupled receptors(GPCRs)play fundamental roles in the human biololgy and drug discovery.GPCRs function as signalling molecules that transduce extracellular signals into cells.The signalling transduction ...The G-protein coupled receptors(GPCRs)play fundamental roles in the human biololgy and drug discovery.GPCRs function as signalling molecules that transduce extracellular signals into cells.The signalling transduction is generally triggered by interacting with ligands,including photons,ions,small organic compounds,peptides,proteins and lipids.In this review,we focus on interactions with diffusible ligands such as hormones and neurotransmitters.We discuss three aspects of the complexity of the GPCR-ligand interactions:functional selectivity of ligands,receptor subtype selectivity of ligands and orphan GPCRs.展开更多
基金supported in part bythe National Institutes of Health(GM67168 to Dr.Yong Duan)computing resources at the National Supercomputing Center TeraGrid(MCB100132 to Dr.Ting Wang and MCA06N028 to Dr.Yong Duan)
文摘The G-protein coupled receptors(GPCRs)play fundamental roles in the human biololgy and drug discovery.GPCRs function as signalling molecules that transduce extracellular signals into cells.The signalling transduction is generally triggered by interacting with ligands,including photons,ions,small organic compounds,peptides,proteins and lipids.In this review,we focus on interactions with diffusible ligands such as hormones and neurotransmitters.We discuss three aspects of the complexity of the GPCR-ligand interactions:functional selectivity of ligands,receptor subtype selectivity of ligands and orphan GPCRs.