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

被引：41

作者：

Rhee, MH ^{[1
]}

Nevo, I ^{[1
]}

Levy, R ^{[1
]}

Vogel, Z ^{[1
]}

机构：

[1] Weizmann Inst Sci, Dept Neurobiol, IL-76100 Rehovot, Israel

来源：

FEBS LETTERS | 2000年 / 466卷 / 2-3期

基金：

以色列科学基金会;

关键词：

cannabinoid CB2 receptor; G protein; site-directed mutagenesis;

D O I：

10.1016/S0014-5793(00)01094-2

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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 studs the role of this motif in CB2 signaling, D mutations (DPY130-132AAA and D130A) markedly reduced binding of cannabinoid agonists, while no significant reduction was observed sith R131A or Y132A. Mutating a (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, (C) 2000 Federation of European Biochemical Societies.

引用

收藏

页码：300 / 304

页数：5

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