Constitutively active G protein-coupled receptor mutants: implications on receptor function and drug action.
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.
Cotecchia
Susanna
S
Institute of Pharmacology and Toxicology, University of Lausanne, Switzerland. Susanna.Cotecchia@ipharm.unil.ch
Fanelli
Francesca
F
Costa
Tommaso
T
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
D043562:Receptors, G-Protein-Coupled