Role of intracellular loops of cannabinoid CB1 receptor in functional interaction with Gα16

FEBS Letters

Current, Lori¹  Drewett, James G¹  Ho, Begonia Y¹ 

[1] Department of Pharmacology, Physiology and Therapeutics, University of North Dakota, Grand Forks, ND 58202, USA

关键词: Gα16;    Cannabinoid CB1 receptor;    Cannabinoid CB2 receptor;    Receptor–Gα coupling;    G protein-coupled receptor;    Mutagenesis;    CP55;    940;    (−)-3-[2-hydroxy-4-(1;    1-dimethylheptyl)phenyl]-4-[3-hydroxypropyl]cyclohexan-1-ol;    WIN55;    212-2;    R(+)-[2;    3-dihydro-5-methyl-3-[(4-morpholinyl)methyl]pyrrolol[1;    2;    3-de]-1;    4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate;   

DOI  :  10.1016/S0014-5793(02)02917-4

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The cannabinoid CB₁ but not the CB₂ receptor was demonstrated to couple via G_α16 to activate phospholipase C after co-expression in COS7 cells. Chimeric CB₁/CB₂ receptors were used as a model to study receptor–G_α16 interaction. Sequences of the second and third intracellular loops and the carboxy-terminus were substituted from the CB₁ into the CB₂ receptor. Only the triple mutant with all three regions replaced activated phospholipase C to a similar extent as the CB₁ receptor, suggesting that all three intracellular regions are required for interacting with G_α16. Several sub-domains within the third intracellular loop were identified for receptor–G_α16 interaction.

【 授权许可】

Unknown