Development of fluorescent probes that target serotonin 5-HT2B receptors

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• dc.contributor.author Azuaje, Jhonnyca
• dc.contributor.author López, Paulaca
• dc.contributor.author Iglesias, Albaca
• dc.contributor.author de la Fuente, Rocío Ailimca
• dc.contributor.author Pérez Rubio, José M.ca
• dc.contributor.author García, Diegoca
• dc.contributor.author Maciej Stępniewski, Tomaszca
• dc.contributor.author García Mera, Xerardoca
• dc.contributor.author Brea, Joséca
• dc.contributor.author Selent, Janaca
• dc.contributor.author Pérez Sala, Doloresca
• dc.contributor.author Castro, Mariánca
• dc.contributor.author Loza, María I.ca
• dc.contributor.author Sotelo, Eddyca
• dc.date.accessioned 2017-11-27T10:12:30Z
• dc.date.available 2017-11-27T10:12:30Z
• dc.date.issued 2017
• dc.description.abstract Some 5-HT2B fluorescent probes were obtained by tagging 1-(2,5-dimethoxy-4-iodophenyl)-propan-2-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.format.mimetype application/pdfca
• dc.identifier.citation Azuaje J, López P, Iglesias A, de la Fuente RA, Pérez-Rubio JM, García D, et al. Development of fluorescent probes that target serotonin 5-HT2B receptors. Sci Rep. 2017 Sep 7;7(1):10765. DOI: 10.1038/s41598-017-11370-2
• dc.identifier.doi http://dx.doi.org/10.1038/s41598-017-11370-2
• dc.identifier.issn 2045-2322
• dc.identifier.uri http://hdl.handle.net/10230/33347
• dc.language.iso eng
• dc.publisher Nature Publishing Groupca
• dc.relation.ispartof Scientific Reports. 2017 Sep 7;7(1):10765
• dc.relation.projectID info:eu-repo/grantAgreement/ES/3PN/SAF2009-13609-C04-03
• dc.relation.projectID info:eu-repo/grantAgreement/ES/1PE/SAF2014-57138-C2-1-R
• dc.rights © 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.accessRights info:eu-repo/semantics/openAccess
• dc.rights.uri http://creativecommons.org/licenses/by/4.0/
• dc.subject.keyword Chemical tools
• dc.subject.keyword Drug discovery and development
• dc.title Development of fluorescent probes that target serotonin 5-HT2B receptorsca
• dc.type info:eu-repo/semantics/article
• dc.type.version info:eu-repo/semantics/publishedVersion