Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cellpermeable fluorescent probe.
dc.contributor.author | Gazzi, Thais | |
dc.contributor.author | Grande Rodríguez, Mª Teresa | |
dc.contributor.author | Nazare, Marc | |
dc.contributor.author | Romero, Julián | |
dc.date.accessioned | 2023-10-17T11:00:32Z | |
dc.date.available | 2023-10-17T11:00:32Z | |
dc.date.issued | 2022 | |
dc.description.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. | spa |
dc.description.extent | 1213 KB | spa |
dc.identifier.doi | 10.1039/d1sc06659e | spa |
dc.identifier.issn | 2041-6520 | spa |
dc.identifier.uri | https://hdl.handle.net/10641/3469 | |
dc.language.iso | eng | spa |
dc.publisher | Chemical Science | spa |
dc.relation.publisherversion | https://pubs.rsc.org/en/content/articlelanding/2022/sc/d1sc06659e | spa |
dc.rights | Atribución-NoComercial-SinDerivadas 3.0 España | * |
dc.rights.accessRights | open access | spa |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/3.0/es/ | * |
dc.title | Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cellpermeable fluorescent probe. | spa |
dc.type | journal article | spa |
dc.type.hasVersion | AM | spa |
dspace.entity.type | Publication | |
relation.isAuthorOfPublication | 6fcd3567-a25a-488d-b36e-9f009ea27ff8 | |
relation.isAuthorOfPublication.latestForDiscovery | 6fcd3567-a25a-488d-b36e-9f009ea27ff8 |
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