大麻素受体
大麻素
非诺贝特
联轴节(管道)
化学
神经科学
受体
药理学
材料科学
医学
心理学
生物化学
兴奋剂
冶金
作者
Tianxin Wang,Wenqin Tang,Zhen Zhao,Ruihua Zhao,Zhenyu Lv,Xuzhen Guo,Quan-Chang Gu,Boxiang Liu,Haoyu Lv,Jiayan Chen,Kui Zhang,Fahui Li,Jiangyun Wang
标识
DOI:10.1002/advs.202306311
摘要
Abstract The G‐protein‐coupled human cannabinoid receptor 1 (CB1) is a promising therapeutic target for pain management, inflammation, obesity, and substance abuse disorders. The structures of CB1‐G i complexes in synthetic agonist‐bound forms have been resolved to date. However, the commercial drug recognition and G q coupling mechanisms of CB1 remain elusive. Herein, the cryo‐electron microscopy (cryo‐EM) structure of CB1‐G q complex, in fenofibrate‐bound form, at near‐atomic resolution, is reported. The structure elucidates the delicate mechanisms of the precise fenofibrate recognition and G q protein coupling by CB1 and will facilitate future drug discovery and design.
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