Biophysical approaches to G protein-coupled receptors: Structure, functionand dynamics

G protein-coupled receptors (GPCR) represent a large family of drug targets for which there is no high-resolution structural information. In order to understand the mechanisms of ligand recognition and receptor activation, th ere is a strong need for novel biophysical methods. In this Perspective we provide an overview of recent experimental approaches used to explore the m olecular architecture and dynamics of GPCR and their interactions with liga nds and G proteins using biophysical, non-crystallographic, methods.