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Fenofibrate Recognition and Gq Protein Coupling Mechanisms of the Human Cannabinoid Receptor CB1.
- Source :
- Advanced Science; 4/10/2024, Vol. 11 Issue 14, p1-8, 8p
- Publication Year :
- 2024
-
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. [ABSTRACT FROM AUTHOR]
- Subjects :
- CANNABINOID receptors
FENOFIBRATE
DRUG discovery
DRUG design
SUBSTANCE abuse
PROTEINS
Subjects
Details
- Language :
- English
- ISSN :
- 21983844
- Volume :
- 11
- Issue :
- 14
- Database :
- Complementary Index
- Journal :
- Advanced Science
- Publication Type :
- Academic Journal
- Accession number :
- 176536525
- Full Text :
- https://doi.org/10.1002/advs.202306311