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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
  • 条目包含文件:
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