Role of the highly conserved Asp‐Arg‐Tyr motif in signal transduction of the CB2 cannabinoid receptor

FEBS Letters

Rhee, Man-Hee¹  Nevo, Igal¹  Vogel, Zvi¹  Levy, Rivka¹ 

[1]Department of Neurobiology, The Weizmann Institute of Science, Rehovot 76100, Israel

关键词: Cannabinoid;    CB2 receptor;    G protein;    Site-directed mutagenesis;   

DOI  :  10.1016/S0014-5793(00)01094-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The DRY motif, at the junction of transmembrane helix 3 and intracellular loop 2 of G protein-coupled receptors, is highly conserved. Mutations were introduced into the CB₂ cannabinoid receptor to study the role of this motif in CB₂ signaling. D mutations (DRY130–132AAA and D130A) markedly reduced binding of cannabinoid agonists, while no significant reduction was observed with R131A or Y132A. Mutating R (R131A) only partially reduced, and mutating Y (Y132A) more efficiently reduced the cannabinoid-induced inhibition of adenylyl cyclase. Thus, in CB₂, D130 is involved in agonist binding, whereas Y seems to have a role in receptor downstream signaling.

【 授权许可】

Unknown