General description
Authors describe the knowledge of GPCR receptor structure and function, the different mechanisms involved in the regulation of GPCR function, and the role of pharmacological chaperones in GPCR folding and maturation. They also present new findings about how GPCR dimerization/ oligomerization modifies the properties of individual receptors and show how recent developments are leading to significant advances in drug discovery, such as the detection of ligands for orphan GPCRs. Also discussed are the most recent developments that could lead to new drug discoveries: role of GPCRs in mediating pain, development of receptor-type selective drugs based on the structural plasticity of receptor activation, and identification of natural ligands of orphan GPCRs (deorphanization) as possible drug targets.