title: Role of intracellular loops of cannabinoid CB(1) receptor in functional interaction with G(alpha16).
abstract: The cannabinoid CB(1) but not the CB(2) receptor was demonstrated to couple via G(alpha16) to activate phospholipase C after co-expression in COS7 cells. Chimeric CB(1)/CB(2) receptors were used as a model to study receptor-G(alpha16) interaction. Sequences of the second and third intracellular loops and the carboxy-terminus were substituted from the CB(1) into the CB(2) receptor. Only the triple mutant with all three regions replaced activated phospholipase C to a similar extent as the CB(1) receptor, suggesting that all three intracellular regions are required for interacting with G(alpha16). Several sub-domains within the third intracellular loop were identified for receptor-G(alpha16) interaction.
authors.affiliation: Department of Pharmacology, Physiology and Therapeutics, University of North Dakota, Grand Forks 58202, USA. ho.begoniay@kendle.com
authors.forename: Begonia Y
authors.initials: BY
authors.lastname: Ho
authors.forename: Lori
authors.initials: L
authors.lastname: Current
authors.forename: James G
authors.initials: JG
authors.lastname: Drewett
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001665:Binding Sites; D019556:COS Cells; D002186:Cannabinoids / Q000378:metabolism*; D002522:Chlorocebus aethiops; D043802:GTP-Binding Protein alpha Subunits, Gq-G11; D020962:Heterotrimeric GTP-Binding Proteins / Q000235:genetics / Q000378:metabolism*; D006801:Humans; D007424:Intracellular Fluid / Q000378:metabolism; D008969:Molecular Sequence Data; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug / Q000235:genetics / Q000378:metabolism*; D017386:Sequence Homology, Amino Acid; D010738:Type C Phospholipases / Q000378:metabolism
chemical_list: D002186:Cannabinoids; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug; D010738:Type C Phospholipases; C112631:G protein alpha 16; D043802:GTP-Binding Protein alpha Subunits, Gq-G11; D020962:Heterotrimeric GTP-Binding Proteins