title: Mutational analysis of the mouse 5-HT7 receptor: importance of the third intracellular loop for receptor-G-protein interaction.
abstract: The mouse serotonin (5-HT) receptor subtype, 5-HT7, belongs to the family of seven transmembrane G-protein-coupled receptors. To identify the structural basis for the coupling of 5-HT7 receptor to G alpha(s) we constructed a number of receptor mutants in which amino acid residues were either substituted or deleted from the second and third intracellular loops. Wild-type and mutant 5-HT7 receptors were expressed in insect cells using the baculovirus vectors. Two mutant receptor species, 5-HT7(E325G) and 5-HT7(K327S), demonstrated markedly impaired abilities to stimulate adenylyl cyclase. The results suggest the importance of the C-terminal region of the third intracellular loop in receptor-G-protein interaction and that specific charged residues, E325 and K327, may play a critical role in this interaction.
authors.affiliation: School of Biological and Molecular Sciences, Oxford Brookes University, UK.
authors.forename: L A
authors.initials: LA
authors.lastname: Obosi
authors.forename: R
authors.initials: R
authors.lastname: Hen
authors.forename: D J
authors.initials: DJ
authors.lastname: Beadle
authors.forename: I
authors.initials: I
authors.lastname: Bermudez
authors.forename: L A
authors.initials: LA
authors.lastname: King
mesh_terms: D000818:Animals; D016367:Baculoviridae / Q000235:genetics; D002460:Cell Line; D003001:Cloning, Molecular; D019204:GTP-Binding Proteins / Q000378:metabolism*; D051379:Mice; D016296:Mutagenesis; D011487:Protein Conformation; D011869:Radioligand Assay; D011985:Receptors, Serotonin / Q000737:chemistry / Q000235:genetics* / Q000378:metabolism; D018411:Spodoptera
chemical_list: D011985:Receptors, Serotonin; C104425:serotonin 7 receptor; D019204:GTP-Binding Proteins