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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^[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
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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-+.
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