Fenofibrate Recognition and Gq Protein Coupling Mechanisms of the Human Cannabinoid Receptor CB1
2024
发表期刊ADVANCED SCIENCE (IF:14.3[JCR-2023],16.3[5-Year])
ISSN2198-3844
EISSN2198-3844
卷号11期号:14
发表状态已发表
DOI10.1002/advs.202306311
摘要

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-Gi complexes in synthetic agonist-bound forms have been resolved to date. However, the commercial drug recognition and Gq coupling mechanisms of CB1 remain elusive. Herein, the cryo-electron microscopy (cryo-EM) structure of CB1-Gq complex, in fenofibrate-bound form, at near-atomic resolution, is reported. The structure elucidates the delicate mechanisms of the precise fenofibrate recognition and Gq protein coupling by CB1 and will facilitate future drug discovery and design. 

关键词Cryo-electron microscopy Cannabinoid receptors Coupling mechanism Fenofibrate Electron microscopes Electron microscopy Medical imaging G protein Gq coupling Human cannabinoid receptor 1 Human cannabinoid receptors Ligand recognition Receptor-1
收录类别SCI ; EI
语种英语
出版者John Wiley and Sons Inc
EI入藏号20240615494188
EI主题词Proteins
EI分类号461.1 Biomedical Engineering ; 746 Imaging Techniques ; 804.1 Organic Compounds
原始文献类型Journal article (JA)
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文献类型期刊论文
条目标识符https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/421479
专题iHuman研究所
生命科学与技术学院_硕士生
生命科学与技术学院_博士生
共同第一作者Tang, Wenqin; Zhao, Ziyi; Zhao, Ran; Lv, Zhenyu
通讯作者Li, Fahui; Wang, Jiangyun
作者单位
1.CAS Key Laboratory of Quantitative Engineering Biology, Institute of Synthetic Biology, Shenzhen Institute of Advanced Technology, Chinese Academy of Sciences, Shenzhen; 518055, China
2.iHuman Institute, ShanghaiTech University, 393 Middle Huaxia Road, Shanghai, Pudong; 201210, China
3.Institute of Biophysics, Chinese Academy of Sciences, 15 Datun Road, Beijing, Chaoyang District; 100101, China
4.School of Life Sciences, University of Chinese Academy of Sciences, Beijing; 100049, China
5.Key Laboratory of Biomacromolecules, Chinese Academy of Sciences, Beijing; 100101, China
第一作者单位iHuman研究所
推荐引用方式
GB/T 7714
Wang, Tianxin,Tang, Wenqin,Zhao, Ziyi,et al. Fenofibrate Recognition and Gq Protein Coupling Mechanisms of the Human Cannabinoid Receptor CB1[J]. ADVANCED SCIENCE,2024,11(14).
APA Wang, Tianxin.,Tang, Wenqin.,Zhao, Ziyi.,Zhao, Ran.,Lv, Zhenyu.,...&Wang, Jiangyun.(2024).Fenofibrate Recognition and Gq Protein Coupling Mechanisms of the Human Cannabinoid Receptor CB1.ADVANCED SCIENCE,11(14).
MLA Wang, Tianxin,et al."Fenofibrate Recognition and Gq Protein Coupling Mechanisms of the Human Cannabinoid Receptor CB1".ADVANCED SCIENCE 11.14(2024).
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