title: Restructuring G-protein- coupled receptor activation.
abstract: G-protein-coupled receptors serve as key signal transduction conduits, linking extracellular inputs with diverse cellular responses. These receptors eluded structural characterization for decades following their identification. A landmark structure of rhodopsin provided a basis for structure-function studies and homology modeling, but advances in receptor biology suffered from a lack of receptor-specific structural insights. The recent explosion in GPCR structures confirms some features predicted by rhodopsin-based models, and more importantly, it reveals unexpected ligand-binding modes and critical aspects of the receptor activation process. The new structures also promise to foster studies testing emerging models for GPCR function such as receptor dimerization and ligand-biased signaling.
authors.affiliation: Department of Biochemistry, Institute for Research in Immunology and Cancer, Université de Montréal, QC, Canada.
authors.forename: Martin
authors.initials: M
authors.lastname: Audet
authors.forename: Michel
authors.initials: M
authors.lastname: Bouvier
mesh_terms: D000818:Animals; D018360:Crystallography, X-Ray; D006801:Humans; D018343:Receptors, Adrenergic, beta-2 / Q000737:chemistry / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry* / Q000378:metabolism*; D012243:Rhodopsin / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D018343:Receptors, Adrenergic, beta-2; D043562:Receptors, G-Protein-Coupled; D012243:Rhodopsin