Agonist-independent regulation of constitutively active G-protein-coupled receptors.
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.
Leurs
R
R
Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Vrije Universiteit, The Netherlands. leurs@chem.vu.nl
Smit
M J
MJ
Alewijnse
A E
AE
Timmerman
H
H
D000818:Animals; D019204:GTP-Binding Proteins / Q000502:physiology*; D006801:Humans; D011956:Receptors, Cell Surface / Q000819:agonists / Q000502:physiology*
D011956:Receptors, Cell Surface; D019204:GTP-Binding Proteins