Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues

Adrenoceptors are G protein-coupled receptors involved in a large variety of physiological processes, also under pathological conditions. This is due in large part to their ubiquitous expression in the body exerting numerous essential functions. Therefore, the possibility to control their activity w...

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Autores: Duran-Corbera, Anna, Font Inglès, Joan|||0000-0001-8416-1909, Faria, Melissa|||0000-0003-1451-4427, Prats, Eva|||0000-0001-7838-2027, Consegal, Marta|||0000-0002-9201-9117, Catena, Juanlo|||0000-0002-2423-5926, Muñoz, Lourdes, Raldúa, Demetrio|||0000-0001-5256-1641, Rodríguez Sinovas, Antonio|||0000-0003-2930-8773, Llebaria, Amadeu|||0000-0002-8200-4827, Rovira, Xavier|||0000-0002-9764-9927
Tipo de recurso: artículo
Fecha de publicación:2022
País:España
Institución:Universitat Autònoma de Barcelona
Repositorio:Dipòsit Digital de Documents de la UAB
Idioma:inglés
OAI Identifier:oai:ddd.uab.cat:292158
Acceso en línea:https://ddd.uab.cat/record/292158
https://dx.doi.org/urn:doi:10.1016/j.isci.2022.105128
Access Level:acceso abierto
Palabra clave:Biochemistry
Biological sciences
Biological sciences research methodologies
Cell biology
Medical biochemistry
Pharmacology
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spelling Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissuesDuran-Corbera, AnnaFont Inglès, Joan|||0000-0001-8416-1909Faria, Melissa|||0000-0003-1451-4427Prats, Eva|||0000-0001-7838-2027Consegal, Marta|||0000-0002-9201-9117Catena, Juanlo|||0000-0002-2423-5926Muñoz, LourdesRaldúa, Demetrio|||0000-0001-5256-1641Rodríguez Sinovas, Antonio|||0000-0003-2930-8773Llebaria, Amadeu|||0000-0002-8200-4827Rovira, Xavier|||0000-0002-9764-9927BiochemistryBiological sciencesBiological sciences research methodologiesCell biologyMedical biochemistryPharmacologyAdrenoceptors are G protein-coupled receptors involved in a large variety of physiological processes, also under pathological conditions. This is due in large part to their ubiquitous expression in the body exerting numerous essential functions. Therefore, the possibility to control their activity with high spatial and temporal precision would constitute a valuable research tool. In this study, we present a caged version of the approved non-selective β-adrenoceptor antagonist carvedilol, synthesized by alkylation of its secondary amine with a coumarin derivative. Introducing this photo-removable group abolished carvedilol physiological effects in cell cultures, mouse isolated perfused hearts and living zebrafish larvae. Only after visible light application, carvedilol was released and the different physiological systems were pharmacologically modulated in a similar manner as the control drug. This research provides a new photopharmacological tool for a wide range of research applications that may help in the development of future precise therapies.Universitat Autònoma de Barcelona 22022-01-0120222022-01-01Articlehttp://purl.org/coar/resource_type/c_6501VoRhttp://purl.org/coar/version/c_970fb48d4fbd8a85info:eu-repo/semantics/articleapplication/pdfhttps://ddd.uab.cat/record/292158https://dx.doi.org/urn:doi:10.1016/j.isci.2022.105128reponame:Dipòsit Digital de Documents de la UABinstname:Universitat Autònoma de BarcelonaInglésengAgencia Estatal de Investigación https://doi.org/10.13039/501100011033 PID2020-120499RB-I00Ministerio de Economía y Competitividad https://doi.org/10.13039/501100003329 SAF2015-74132-JINopen accesshttp://purl.org/coar/access_right/c_abf2Aquest document està subjecte a una llicència d'ús Creative Commons. Es permet la reproducció total o parcial, la distribució, i la comunicació pública de l'obra, sempre que no sigui amb finalitats comercials, i sempre que es reconegui l'autoria de l'obra original. No es permet la creació d'obres derivades.https://creativecommons.org/licenses/by-nc-nd/4.0/info:eu-repo/semantics/openAccessoai:ddd.uab.cat:2921582026-06-06T12:50:31Z
dc.title.none.fl_str_mv Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues
title Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues
spellingShingle Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues
Duran-Corbera, Anna
Biochemistry
Biological sciences
Biological sciences research methodologies
Cell biology
Medical biochemistry
Pharmacology
title_short Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues
title_full Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues
title_fullStr Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues
title_full_unstemmed Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues
title_sort Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues
dc.creator.none.fl_str_mv Duran-Corbera, Anna
Font Inglès, Joan|||0000-0001-8416-1909
Faria, Melissa|||0000-0003-1451-4427
Prats, Eva|||0000-0001-7838-2027
Consegal, Marta|||0000-0002-9201-9117
Catena, Juanlo|||0000-0002-2423-5926
Muñoz, Lourdes
Raldúa, Demetrio|||0000-0001-5256-1641
Rodríguez Sinovas, Antonio|||0000-0003-2930-8773
Llebaria, Amadeu|||0000-0002-8200-4827
Rovira, Xavier|||0000-0002-9764-9927
author Duran-Corbera, Anna
author_facet Duran-Corbera, Anna
Font Inglès, Joan|||0000-0001-8416-1909
Faria, Melissa|||0000-0003-1451-4427
Prats, Eva|||0000-0001-7838-2027
Consegal, Marta|||0000-0002-9201-9117
Catena, Juanlo|||0000-0002-2423-5926
Muñoz, Lourdes
Raldúa, Demetrio|||0000-0001-5256-1641
Rodríguez Sinovas, Antonio|||0000-0003-2930-8773
Llebaria, Amadeu|||0000-0002-8200-4827
Rovira, Xavier|||0000-0002-9764-9927
author_role author
author2 Font Inglès, Joan|||0000-0001-8416-1909
Faria, Melissa|||0000-0003-1451-4427
Prats, Eva|||0000-0001-7838-2027
Consegal, Marta|||0000-0002-9201-9117
Catena, Juanlo|||0000-0002-2423-5926
Muñoz, Lourdes
Raldúa, Demetrio|||0000-0001-5256-1641
Rodríguez Sinovas, Antonio|||0000-0003-2930-8773
Llebaria, Amadeu|||0000-0002-8200-4827
Rovira, Xavier|||0000-0002-9764-9927
author2_role author
author
author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Universitat Autònoma de Barcelona
dc.subject.none.fl_str_mv Biochemistry
Biological sciences
Biological sciences research methodologies
Cell biology
Medical biochemistry
Pharmacology
topic Biochemistry
Biological sciences
Biological sciences research methodologies
Cell biology
Medical biochemistry
Pharmacology
description Adrenoceptors are G protein-coupled receptors involved in a large variety of physiological processes, also under pathological conditions. This is due in large part to their ubiquitous expression in the body exerting numerous essential functions. Therefore, the possibility to control their activity with high spatial and temporal precision would constitute a valuable research tool. In this study, we present a caged version of the approved non-selective β-adrenoceptor antagonist carvedilol, synthesized by alkylation of its secondary amine with a coumarin derivative. Introducing this photo-removable group abolished carvedilol physiological effects in cell cultures, mouse isolated perfused hearts and living zebrafish larvae. Only after visible light application, carvedilol was released and the different physiological systems were pharmacologically modulated in a similar manner as the control drug. This research provides a new photopharmacological tool for a wide range of research applications that may help in the development of future precise therapies.
publishDate 2022
dc.date.none.fl_str_mv 2
2022-01-01
2022
2022-01-01
dc.type.none.fl_str_mv Article
http://purl.org/coar/resource_type/c_6501
VoR
http://purl.org/coar/version/c_970fb48d4fbd8a85
dc.type.openaire.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv https://ddd.uab.cat/record/292158
https://dx.doi.org/urn:doi:10.1016/j.isci.2022.105128
url https://ddd.uab.cat/record/292158
https://dx.doi.org/urn:doi:10.1016/j.isci.2022.105128
dc.language.none.fl_str_mv Inglés
eng
language_invalid_str_mv Inglés
language eng
dc.relation.none.fl_str_mv Agencia Estatal de Investigación https://doi.org/10.13039/501100011033 PID2020-120499RB-I00
Ministerio de Economía y Competitividad https://doi.org/10.13039/501100003329 SAF2015-74132-JIN
dc.rights.none.fl_str_mv open access
http://purl.org/coar/access_right/c_abf2
https://creativecommons.org/licenses/by-nc-nd/4.0/
dc.rights.openaire.fl_str_mv info:eu-repo/semantics/openAccess
rights_invalid_str_mv open access
http://purl.org/coar/access_right/c_abf2
https://creativecommons.org/licenses/by-nc-nd/4.0/
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv reponame:Dipòsit Digital de Documents de la UAB
instname:Universitat Autònoma de Barcelona
instname_str Universitat Autònoma de Barcelona
reponame_str Dipòsit Digital de Documents de la UAB
collection Dipòsit Digital de Documents de la UAB
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