8K8J

Cannabinoid Receptor 1 bound to Fenofibrate coupling MiniGsq and Nb35 Complex

Summary for 8K8J

• Entry DOI: 10.2210/pdb8k8j/pdb
• EMDB information: 36951
• Descriptor: Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... (6 entities in total)
• Functional Keywords: gpcr, membrane protein
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 5
• Total formula weight: 153885.58

Authors

Tang, W.Q.,Wang, T.X.,Li, F.H.,Wang, J.Y. (deposition date: 2023-07-30, release date: 2024-02-14, Last modification date: 2025-07-23)

Primary citation

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.
Fenofibrate Recognition and G q Protein Coupling Mechanisms of the Human Cannabinoid Receptor CB1.
Adv Sci, 11:e2306311-e2306311, 2024

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 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.

PubMed: 38298116
DOI: 10.1002/advs.202306311

Experimental method

ELECTRON MICROSCOPY (2.88 Å)