title: Constitutively active G protein-coupled receptor mutants: implications on receptor function and drug action.
abstract: Mutations of GPCRs can increase their constitutive (agonist-independent) activity. Some of these mutations have been artificially introduced by site-directed mutagenesis; others occur spontaneously in human diseases. The analysis of constitutively active GPCR mutants has attracted a large interest in the past decade, providing an important contribution to our understanding of the molecular mechanisms underlying receptor function and drug action.
authors.affiliation: Institute of Pharmacology and Toxicology, University of Lausanne, Switzerland. Susanna.Cotecchia@ipharm.unil.ch
authors.forename: Susanna
authors.initials: S
authors.lastname: Cotecchia
authors.forename: Francesca
authors.initials: F
authors.lastname: Fanelli
authors.forename: Tommaso
authors.initials: T
authors.lastname: Costa
mesh_terms: D004358:Drug Therapy / Q000639:trends*; D005544:Forecasting; D016297:Mutagenesis, Site-Directed; D009154:Mutation; D043562:Receptors, G-Protein-Coupled / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism
chemical_list: D043562:Receptors, G-Protein-Coupled