A comprehensive survey of the many recent advances in the field of G protein-coupled receptors (GPCR). The authors describe the current 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: the role of GPCRs in mediating pain, the development of receptor-type selective drugs based on the structural plasticity of receptor activation, and the identification of natural ligands of orphan GPCRs (deorphanization) as possible drug targets.

Includes supplementary material: sn.pub/extras

Inhalt
GPCRs: Structure and Function.- StructureFunction Relationships in G Protein-Coupled Receptors.- Molecular Mechanisms Involved in the Activation of Rhodopsin-Like Seven-Transmembrane Receptors.- GPCR Folding and Maturation.- Regulated Membrane Trafficking and Proteolysis of GPCRs.- GPCR Activity and Its Regulators.- Heterotrimeric G Proteins and Their Effector Pathways.- RGS Proteins.- G Protein-Coupled Receptor Kinases.- Regulators of GPCR Activity.- GPCR Interacting Proteins.- GPCR Dimerization/Oligomerization.- Biophysical and Biochemical Methods to Study GPCR Oligomerization.- Oligomerization Domains of G Protein-Coupled Receptors.- Functional Complementation and the Analysis of GPCR Dimerization.- The Role of Oligomerization in G Protein-Coupled Receptor Maturation.- Receptor Oligomerization and Trafficking.- Modulation of Receptor Pharmacology by G Protein-Coupled Receptor Dimerization.- Recent Developments in Drug Discovery.- Role of Heteromeric GPCR Interactions in Pain/Analgesia.- Conformational Plasticity of GPCR Binding Sites.- De-Orphanizing GPCRs and Drug Development.