Leiden University Scholarly Publications

Paus, L.V. de; Yu, A.; Janssen, A.P.A.; Berg, R.J.B.H.N. van den; Heitman, L.H.; Stelt, M. van der (2024)

Discovery of a photoaffinity probe that captures the active conformation of the cannabinoid CB2 receptor

Article / Letter to editor

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.

All authors

Paus, L.V. de; Yu, A.; Janssen, A.P.A.; Berg, R.J.B.H.N. van den; Heitman, L.H.; Stelt, M. van der

Date

2024-04-02

Journal

ChemBioChem

Volume

25

Issue

7

DOI

doi:10.1002/cbic.202300785