Genetically Encoded CB2R-Based Fluorescent Sensor Enables Rapid Screening and Functional Assessment of Cannabinoid Modulators
The G-protein-coupled receptor cannabinoid receptor 2 (CB<sub>2</sub>R) initiates a key signaling pathway in mammalian physiology and pathophysiology. CB<sub>2</sub>R signaling holds significant therapeutic potential in ameliorating many pathologies, particularly in inflammatory conditions, neurodegenerative disorders, fibroproliferative and ocular diseases. CB2 modulators have been studied for their anti-inflammatory and tissue protective effects in preclinical animal models of cardiovascular, gastrointestinal, liver, kidney, lung and neurodegenerative disorders with numerous compounds undergoing clinical evaluation. Existing ligands can be classified as endocannabinoids, cannabinoid-like natural products and synthetic CB<sub>2</sub>R ligands. A genetically encoded G-protein-coupled receptor activation-based (GRAB) sensor for CB<sub>1</sub>R-GRAB<sub>eCB2.0</sub> was developed recently. This current study extends the sensor's development to allow for a GPCR activation-based sensor for CB<sub>2</sub>R. The sensor, GRAB-CB2, will facilitate the evaluation of pharmacological characteristics and responses of various functionally selective and indiscriminate cannabinoid ligands acting on CB2.
Authors
- Malliga R. Iyer (ORCID: https://orcid.org/0000-0002-0116-4619)
- Henry L. Puhl (ORCID: https://orcid.org/0000-0003-3095-7201)
- Samay Shivshankar
- Pinaki Bhattacharjee (ORCID: https://orcid.org/0000-0003-1818-3610)
- Paul Volesky
Institutions
- National Institutes of Health (US)
- National Institute on Alcohol Abuse and Alcoholism (US)
Publication Details
- Journal
- International Journal of Molecular Sciences
- Published
- 2026-02-24
- DOI
- https://doi.org/10.3390/ijms27052095
- Primary Topic
- Cannabis and Cannabinoid Research
- Type
- article
- Field-Weighted Citation Impact
- 0.00