Functional roles of the tyrosine within the NP(X) n Y motif and the cysteines in the C‐terminal juxtamembrane region of the CB2 cannabinoid receptor

FEBS Letters

Feng, Wenke¹  Song, Z.H¹ 

[1] Department of Pharmacology and Toxicology, University of Louisville School of Medicine, Louisville, KY 40292, USA

关键词: Cannabinoid receptor 2;    Cannabinoid;    Site-directed mutagenesis;    Structure;    Function;   

DOI  :  10.1016/S0014-5793(01)02642-4

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

In G protein-coupled receptors, a NP(X) _n Y motif in the seventh transmembrane domain and cysteine residues in the C-terminal juxtamembrane region are conserved. In the current study, the roles of Y299 within the NPVIY motif and C313 and C320 in the C-terminal juxtamembrane region of the human CB2 cannabinoid receptor were investigated by site-directed mutagenesis. Replacing Y299 with alanine resulted in a complete loss of ligand binding and a severe impairment of cannabinoid-induced inhibition of forskolin-stimulated cAMP accumulation. The C313A and C320A mutations markedly reduced functional coupling to adenylate cyclase, but had no effect on ligand binding and agonist-induced receptor desensitization.

【 授权许可】

Unknown