Constitutively active G protein-coupled receptors: potential mechanisms of receptor activation.
Mutations of G protein-coupled receptors 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 the constitutively active G protein-coupled receptors has provided important informations about the molecular mechanisms underlying receptor activation and drug action.
Scheer
A
A
Institut de Pharmacologie et de Toxicologie Université de Lausanne, Switzerland.
Cotecchia
S
S
D019204:GTP-Binding Proteins; D006801:Humans; D007536:Isomerism; D008958:Models, Molecular; D016297:Mutagenesis, Site-Directed; D011956:Receptors, Cell Surface / Q000235:genetics / Q000378:metabolism*
D011956:Receptors, Cell Surface; D019204:GTP-Binding Proteins