Fenofibrate Recognition and G q Protein Coupling Mechanisms of the Human Cannabinoid Receptor CB1

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 complexes in synthetic agonist-bound forms have been resolved to date. However, the commercial drug recognitio...

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Bibliographic Details
Published in:Advanced science 2024-04, Vol.11 (14), p.e2306311
Main Authors: Wang, Tianxin, Tang, Wenqin, Zhao, Ziyi, Zhao, Ran, Lv, Zhenyu, Guo, Xuzhen, Gu, Quanchang, Liu, Boxiang, Lv, Haoyu, Chen, Jiayan, Zhang, Kaiquan, Li, Fahui, Wang, Jiangyun
Format: Article
Language:English
Subjects:
Cannabinoids
Cryoelectron Microscopy
Fenofibrate
GTP-Binding Proteins
Humans
Receptor, Cannabinoid, CB1
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Summary: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 complexes in synthetic agonist-bound forms have been resolved to date. However, the commercial drug recognition and G coupling mechanisms of CB1 remain elusive. Herein, the cryo-electron microscopy (cryo-EM) structure of CB1-G complex, in fenofibrate-bound form, at near-atomic resolution, is reported. The structure elucidates the delicate mechanisms of the precise fenofibrate recognition and G protein coupling by CB1 and will facilitate future drug discovery and design.
ISSN:2198-3844
2198-3844
DOI:10.1002/advs.202306311