title: Agonist-independent regulation of constitutively active G-protein-coupled receptors.
abstract: G-protein-coupled receptors constitute one of the largest protein super-families in mammals. Since the cloning of the encoding genes, these important drug targets have been subjected to thorough biochemical and pharmacological studies. It has become clear that G-protein-coupled receptors not only transmit signals after stimulation by agonists but can also spontaneously couple to signal-transduction pathways. Recent findings show that constitutively active G-protein-coupled receptors can also be regulated in an agonist-independent manner, which has important implications for the interpretation of the actions of (inverse) agonists and the results of site-directed-mutagenesis studies.
authors.affiliation: Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Vrije Universiteit, The Netherlands. leurs@chem.vu.nl
authors.forename: R
authors.initials: R
authors.lastname: Leurs
authors.forename: M J
authors.initials: MJ
authors.lastname: Smit
authors.forename: A E
authors.initials: AE
authors.lastname: Alewijnse
authors.forename: H
authors.initials: H
authors.lastname: Timmerman
mesh_terms: D000818:Animals; D019204:GTP-Binding Proteins / Q000502:physiology*; D006801:Humans; D011956:Receptors, Cell Surface / Q000819:agonists / Q000502:physiology*
chemical_list: D011956:Receptors, Cell Surface; D019204:GTP-Binding Proteins