G protein-coupled receptors (GPCRs) are transmembrane proteins that transduce an extracellular signal—ligand binding—into an intracellular signal—activation of G-protein—which in turn activates ...

GPCRs are the targets for around one third of all approved drugs 1. Yet such medicines act on only a handful of the 800+ known GPCRs. A wave of biomedical progress in the early 21 st century thrust ...