摘要
G-protein coupled receptors （GPCRs） play essential roles in signal transduction from the environment into the cell. While many structural features have been elu- cidated in great detail, a common functional mechanism on how the ligand-binding signal is converted into a conformational change on the cytoplasmic face result- ing in subsequent activation of downstream effectors remain to be established. Based on available structural and functional data of the activation process in class-A GPCRs, we propose here that a change in protonation status, together with proton transfer via conserved structural elements located in the transmembrane region, are the key elements essential for signal trans- duction across the membrane.
G-protein coupled receptors （GPCRs） play essential roles in signal transduction from the environment into the cell. While many structural features have been elu- cidated in great detail, a common functional mechanism on how the ligand-binding signal is converted into a conformational change on the cytoplasmic face result- ing in subsequent activation of downstream effectors remain to be established. Based on available structural and functional data of the activation process in class-A GPCRs, we propose here that a change in protonation status, together with proton transfer via conserved structural elements located in the transmembrane region, are the key elements essential for signal trans- duction across the membrane.
