Discovery of a Photoaffinity Probe that Captures the Active Conformation of the Cannabinoid CB2 Receptor.
Chembiochem
; 25(7): e202300785, 2024 Apr 02.
Article
in En
| MEDLINE
| ID: mdl-38372466
ABSTRACT
The cannabinoid receptor type 2 (CB2R) is a G protein-coupled receptor with therapeutic potential for the treatment of inflammatory disorders. Fluorescent probes are desirable to study its receptor localization, expression and occupancy. Previously, we have reported a photoaffinity probe LEI-121 that stabilized the inactive conformation of the CB2R. Here, we report the structure-based design of a novel bifunctional probe that captures the active conformation of the CB2R upon irradiation with light. An alkyne handle was incorporated to visualize the receptor using click-chemistry with fluorophore-azides. These probes may hold promise to study different receptor conformations in relation to their cellular localization and function.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Cannabinoids
/
Fluorescent Dyes
Language:
En
Journal:
Chembiochem
Journal subject:
BIOQUIMICA
Year:
2024
Document type:
Article
Affiliation country:
Netherlands
Country of publication:
Germany