Binding the receptor at both ends

摘要

G-protein-coupled receptors (GPCRs) constitute a large family of proteins -consisting of more than 800 members in humans - that are embedded in the plasma membranes of most cells. They bind specifi-cally to a diverse range of'agonist' molecules, which convey sensory information or commu-nicate changes in physiological states1. Once stimulated by agonists, GPCRs bind to and activate G proteins, which are attached to the inner surface of cell membranes. The G pro-teins then initiate signal cascades that control a wide variety of important biological processes. In this issue, two papers from Kobilka and col-leagues2'3 and another from the groups of Tate and Schertler4 report structural, biophysical and computational studies that provide insight into GPCR activation by agonists.