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http://hdl.handle.net/10261/347419
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dc.contributor.author | Dumazer, Anaëlle | es_ES |
dc.contributor.author | Gómez-Santacana, Xavier | es_ES |
dc.contributor.author | Malhaire, Fanny | es_ES |
dc.contributor.author | Jopling, Chris | es_ES |
dc.contributor.author | Maurel, Damien | es_ES |
dc.contributor.author | Lebon, Guillaume | es_ES |
dc.contributor.author | Llebaria, Amadeu | es_ES |
dc.contributor.author | Goudet, Cyril | es_ES |
dc.date.accessioned | 2024-02-19T09:50:40Z | - |
dc.date.available | 2024-02-19T09:50:40Z | - |
dc.date.issued | 2024-02-07 | - |
dc.identifier.citation | ACS Chemical Neurosciesce 15 (3): 645–655 (2024) | es_ES |
dc.identifier.uri | http://hdl.handle.net/10261/347419 | - |
dc.description.abstract | In recent years, there has been growing interest in the potential therapeutic use of inhibitors of adenosine A2A receptors (A2AR) for the treatment of neurodegenerative diseases and cancer. Nevertheless, the widespread expression of A2AR throughout the body emphasizes the importance of temporally and spatially selective ligands. Photopharmacology is an emerging strategy that utilizes photosensitive ligands to attain high spatiotemporal precision and regulate the function of biomolecules using light. In this study, we combined photochemistry and cellular and in vivo photopharmacology to investigate the light sensitivity of the FDA-approved antagonist istradefylline and its potential use as an A2AR photopharmacological tool. Our findings reveal that istradefylline exhibits rapid trans-to-cis isomerization under near-UV light, and prolonged exposure results in the formation of photocycloaddition products. We demonstrate that exposure to UV light triggers a time-dependent decrease in the antagonistic activity of istradefylline in A2AR-expressing cells and enables real-time optical control of A2AR signaling in living cells and zebrafish. Together, these data demonstrate that istradefylline is a photoinactivatable A2AR antagonist and that this property can be utilized to perform photopharmacological experiments in living cells and animals. | es_ES |
dc.description.sponsorship | The authors thank Gavin Fergusson for helpful discussions and critical reading the manuscript, Lourdes Muñoz from SIMChem (IQAC CSIC) for the use of analytical support and helpful discussions, Fabrice Dubois and Stephane Bedut for the development of the custom illumination module for the FDSS/μCELL plate image and the staff of Montpellier Biocampus facilities for their technical help: the PVM facility for the preparation of lentivirus, the Arpege facility for cell-based pharmacological experiments, and the Zefix facility for zebrafish experiments. This work was publicly funded through ANR (the French National Research Agency) under the “Investissements d’avenir” program I-Site MUSE with the reference ANR-16-IDEX-0006 to A.D. and C.G., and the reference ANR-20-CE11-019 to G.L. This work was supported by the Fondation pour la Recherche Médicale, grant number “MND202003011477”, to C.G. These results have received funding from European Union’s Horizon 2020 research and innovation programme under Marie Skłodowska-Curie grant agreement no. 801342 (Tecniospring INDUSTRY, TECSPR19-1-0062) and the Government of Catalonia’s Agency for Business Competitiveness (ACCIÓ) to XGS, Ministerio de Ciencia e Innovación, Agencia Estatal de Investigación and ERDF─A way of making Europe (PCI2018-093047, PID2020-120499RB-I00) to A.L., and the Catalan government (2021 SGR 00508) to A.L. The illustrative graphics were created with http://biorender.com/. | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | American Chemical Society | es_ES |
dc.relation.ispartof | ACS chemical neuroscience | es_ES |
dc.relation.isversionof | Postprint | es_ES |
dc.rights | embargoedAccess | es_ES |
dc.subject | Purinergic | es_ES |
dc.subject | GPCR | es_ES |
dc.subject | Adenosine | es_ES |
dc.subject | Photopharmacology | es_ES |
dc.subject | Photoswitch | es_ES |
dc.title | Optical Control of Adenosine A2A Receptor Using Istradefylline Photosensitivity | es_ES |
dc.type | artículo | es_ES |
dc.identifier.doi | 10.1021/acschemneuro.3c00721 | - |
dc.description.peerreviewed | Peer reviewed | es_ES |
dc.relation.publisherversion | https://doi.org/10.1021/acschemneuro.3c00721 | es_ES |
dc.embargo.terms | 2025-01-26 | es_ES |
dc.relation.csic | Sí | es_ES |
oprm.item.hasRevision | no ko 0 false | * |
dc.contributor.orcid | 0000-0001-8830-0494 | es_ES |
dc.contributor.orcid | 0000-0002-8255-3535 | es_ES |
dc.identifier.pmid | 38275568 | - |
dc.identifier.scopus | 2-s2.0-85184519810 | - |
dc.identifier.url | https://api.elsevier.com/content/abstract/scopus_id/85184519810 | - |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
dc.subject.sdg | Ensure healthy lives and promote well-being for all at all ages | es_ES |
item.cerifentitytype | Publications | - |
item.languageiso639-1 | en | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.grantfulltext | embargo_20250126 | - |
item.fulltext | With Fulltext | - |
item.openairetype | artículo | - |
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cn3c00721_si_001.pdf.crdownload | Material suplementario | 2,36 MB | Unknown | Visualizar/Abrir |
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