Activation mechanisms of G-protein-coupled receptors based on the structural dynamics

点击翻译按钮获取中文摘要

The activation process of G protein-coupled receptors was investigated based on the structural dynamics using rhodopsin. The effect of the ligand on the structure and equilibrium of the active state was analyzed by high-angle solution X-ray scattering, single-molecule fluorometry, and Fourier-transform infrared spectroscopy. Our results demonstrated that G protein-coupled receptors are in the equilibrium between active and inactive conformations, and the inverse-agonist and agonist bias the equilibrium toward inactive and active conformations, respectively, to regulate the activity.