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-Structure paper
Title | Fenofibrate Recognition and G Protein Coupling Mechanisms of the Human Cannabinoid Receptor CB1. |
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Journal, issue, pages | Adv Sci (Weinh), Vol. 11, Issue 14, Page e2306311, Year 2024 |
Publish date | Jan 31, 2024 |
Authors | Tianxin Wang / Wenqin Tang / Ziyi Zhao / Ran Zhao / Zhenyu Lv / Xuzhen Guo / Quanchang Gu / Boxiang Liu / Haoyu Lv / Jiayan Chen / Kaiquan Zhang / Fahui Li / Jiangyun Wang / |
PubMed 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 complexes ...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. |
External links | Adv Sci (Weinh) / PubMed:38298116 / PubMed Central |
Methods | EM (single particle) |
Resolution | 2.88 - 3.05 Å |
Structure data | EMDB-36951, PDB-8k8j: EMDB-36952: Cannabinoid Receptor 1 bound to Fenofibrate coupling MiniGsq and Nb35 Complex-Global Refine EMDB-36953: Cannabinoid Receptor 1 bound to Fenofibrate coupling MiniGsq and Nb35 Complex-Local Refine |
Chemicals |
ChemComp-J3O: |
Source |
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Keywords | MEMBRANE PROTEIN / GPCR |