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Journal Article

Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe

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Sarott,  Roman C.
Chemical Biology, Max Planck Institute for Medical Research, Max Planck Society;

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https://pubs.rsc.org/en/content/articlelanding/2022/sc/d1sc06659e
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Citation

Gazzi, T., Brennecke, B., Atz, K., Korn, C., Sykes, D., Forn-Cuni, G., et al. (2022). Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe. Chemical Science, 13(19), 5539-5545. doi:10.1039/d1sc06659e.


Cite as: https://hdl.handle.net/21.11116/0000-000F-F38F-E
Abstract
Despite its essential role in the (patho)physiology of several diseases, CB2R tissue expression profiles and signaling mechanisms are not yet fully understood. We report the development of a highly potent, fluorescent CB2R agonist probe employing structure-based reverse design. It commences with a highly potent, preclinically validated ligand, which is conjugated to a silicon-rhodamine fluorophore, enabling cell permeability. The probe is the first to preserve interspecies affinity and selectivity for both mouse and human CB2R. Extensive cross-validation (FACS, TR-FRET and confocal microscopy) set the stage for CB2R detection in endogenously expressing living cells along with zebrafish larvae. Together, these findings will benefit clinical translatability of CB2R based drugs.