EMD-36951
Cannabinoid Receptor 1 bound to Fenofibrate coupling MiniGsq and Nb35 Complex
EMD-36951
Composite mapSingle-particle
2.88 Å
Deposition: 30/07/2023Map released: 14/02/2024
Last modified: 20/11/2024
Sample Organism:
Homo sapiens
Sample: Cannabinoid Receptor 1-G protein complex
Fitted models: 8k8j (Avg. Q-score: 0.534)
Raw data: EMPIAR-11642
Deposition Authors: Tang WQ, Wang TX, Li FH, Wang JY
Sample: Cannabinoid Receptor 1-G protein complex
Fitted models: 8k8j (Avg. Q-score: 0.534)
Raw data: EMPIAR-11642
Deposition Authors: Tang WQ, Wang TX, Li FH, Wang JY
Fenofibrate Recognition and G q Protein Coupling Mechanisms of the Human Cannabinoid Receptor CB1.
Wang T,
Tang W,
Zhao Z,
Zhao R,
Lv Z,
Guo X,
Gu Q,
Liu B,
Lv H,
Chen J,
Zhang K,
Li F 
,
Wang J
(2024) Adv Sci , 11 , e2306311 - e2306311
,
Wang J
(2024) Adv Sci , 11 , e2306311 - e2306311
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-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.
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.