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dc.contributor.author | Azuaje Guerrero, Jhonny Alberto |
dc.contributor.author | López, Paula |
dc.contributor.author | Iglesias Fernández, Alba |
dc.contributor.author | Fuente, Rocío de la |
dc.contributor.author | Pérez Rubio, José M. |
dc.contributor.author | García Peña, Diego |
dc.contributor.author | Stępniewski, Tomasz Maciej |
dc.contributor.author | García Mera, Xerardo Xusto |
dc.contributor.author | Brea Floriani, José Manuel |
dc.contributor.author | Selent, Jana |
dc.contributor.author | Pérez Meirás, María Dolores |
dc.contributor.author | Castro Pérez, María de los Ángeles |
dc.contributor.author | Loza García, María Isabel |
dc.contributor.author | Sotelo Pérez, Eddy |
dc.date.accessioned | 2020-05-24T20:18:29Z |
dc.date.available | 2020-05-24T20:18:29Z |
dc.date.issued | 2017 |
dc.identifier.citation | Azuaje, J., López, P., Iglesias, A. et al. Development of Fluorescent Probes that Target Serotonin 5-HT2B Receptors. Sci Rep 7, 10765 (2017). https://doi.org/10.1038/s41598-017-11370-2 |
dc.identifier.uri | http://hdl.handle.net/10347/22518 |
dc.description.abstract | Some 5-HT2B fluorescent probes were obtained by tagging 1-(2,5-dimethoxy-4-iodophenyl)-propan2-amine (DOI) with a subset of fluorescent amines. Some of the resulting fluorescent ligands showed excellent affinity and selectivity profiles at the 5-HT2B receptors (e.g. 12b), while retain the agonistic functional behaviour of the model ligand (DOI). The study highlighted the most salient features of the structure-activity relationship in this series and these were substantiated by a molecular modelling study based on a receptor-driven docking model constructed on the basis of the crystal structure of the human 5-HT2B receptor. One of the fluorescent ligands developed in this work, compound 12i, specifically labelled CHO-K1 cells expressing 5-HT2B receptors and not parental CHO-K1 cells in a concentration-dependent manner. 12i enables imaging and quantification of specific 5-HT2B receptor labelling in live cells by automated fluorescence microscopy as well as quantification by measurements of fluorescence intensity using a fluorescence plate reader. |
dc.description.sponsorship | This research was carried out within the framework of the Cost Action GLISTEN and financially supported by the Spanish Government (grant numbers SAF2009-13609-C04-03 and GPC2014/003 (PS09/63) to E.S. and SAF2014- 57138-C2-1-R to M.C. and M.I.L.). Authors also thanks financial support from Consellería de Cultura, Educación e Ordenación Universitaria of the Galician Government: (grant: GPC2014/03), Centro Singular de Investigación de Galicia accreditation 2016-2019 (ED431G/09). J. S. acknowledges financial support from Instituto de Salud Carlos III FEDER (CP12/03139 and PI15/00460) |
dc.language.iso | eng |
dc.publisher | Nature Publishing Group |
dc.rights | © The Author(s) 2017. Open Access. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/ |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ |
dc.title | Development of fluorescent probes that target serotonin 5-HT2B receptors |
dc.type | journal article |
dc.identifier.doi | 10.1038/s41598-017-11370-2 |
dc.relation.publisherversion | https://doi.org/10.1038/s41598-017-11370-2 |
dc.type.hasVersion | VoR |
dc.identifier.essn | 2045-2322 |
dc.rights.accessRights | open access |
dc.contributor.affiliation | Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas |
dc.contributor.affiliation | Universidade de Santiago de Compostela. Centro de Investigación en Química Biolóxica e Materiais Moleculares |
dc.contributor.affiliation | Universidade de Santiago de Compostela. Departamento de Química Orgánica |
dc.description.peerreviewed | SI |
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© The Author(s) 2017. Open Access. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/
© The Author(s) 2017. Open Access. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/