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Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-G(i) Complex Structures 期刊论文 WOS高被引论文

编号：

9FBE7DE79DF8496007D4BD8285E7ECA5
作者：

Hua, Tian(华甜)#*^[1]Li, Xiaoting#^[1]Wu, Lijie#^[1]IliopoulosTsoutsouvas, Christos^[2,3];Wang, Yuxia^[1];Wu, Meng^[1,4];Shen, Ling^[1,4];Johnston, Christina A.;Nikas, Spyros P.^[2,3];Song, Feng^[7];Song, Xiyong^[8];Yuan, Shuguang^[9]Sun, Qianqian^[1];Wu, Yiran^[1]Jiang, Shan^[2,3];Grim, Travis W.^[5,6];Benchama, Othman^[2,3];Stahl, Edward L.^[5,6];Zvonok, Nikolai^[2,3];Zhao, Suwen(赵素文)^[1,4]Bohn, Laura M.^[5,6]Makriyannis, Alexandros^[2,10,11]Liu, ZhiJie(刘志杰)*^[1,4,8]
语种：

英文
期刊：

CELL ISSN：0092-8674 2020 年 180 卷 4 期 (655 - +) ; FEB 20
收录：
摘要：

Human endocannabinoid systems modulate multiple physiological processes mainly through the activation of cannabinoid receptors CB1 and CB2. Their high sequence similarity, low agonist selectivity, and lack of activation and G protein-coupling knowledge have hindered the development of therapeutic applications. Importantly, missing structural information has significantly held back the development of promising CB2-selective agonist drugs for treating inflammatory and neuropathic pain without the psychoactivity of CB1. Here, we report the cryoelectron microscopy structures of synthetic cannabinoid-bound CB2 and CB1 in complex with G(i), as well as agonist-bound CB2 crystal structure. Of important scientific and therapeutic benefit, our results reveal a diverse activation and signaling mechanism, the structural basis of CB2-selective agonists design, and the unexpected interaction of cholesterol with CB1, suggestive of its endogenous allosteric modulating role.
推荐引用方式
GB/T 7714：

Hua Tian,Li Xiaoting,Wu Lijie, et al. Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-G(i) Complex Structures [J].CELL,2020,180(4):655-+.
APA：

Hua Tian,Li Xiaoting,Wu Lijie,Iliopoulos-Tsoutsouvas Christos,&Liu Zhi-Jie.(2020).Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-G(i) Complex Structures .CELL,180(4):655-+.
MLA：

Hua Tian, et al. "Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-G(i) Complex Structures" .CELL 180,4(2020):655-+.
入库时间：

2020/4/13 14:46:51
更新时间：

2020/4/13 14:46:51
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