Mostrar o rexistro simple do ítem

dc.contributor.authorAzuaje Guerrero, Jhonny Alberto
dc.contributor.authorLópez, Paula
dc.contributor.authorIglesias Fernández, Alba
dc.contributor.authorFuente, Rocío de la
dc.contributor.authorPérez Rubio, José M.
dc.contributor.authorGarcía Peña, Diego
dc.contributor.authorStępniewski, Tomasz Maciej
dc.contributor.authorGarcía Mera, Xerardo Xusto
dc.contributor.authorBrea Floriani, José Manuel
dc.contributor.authorSelent, Jana
dc.contributor.authorPérez Meirás, María Dolores
dc.contributor.authorCastro Pérez, María de los Ángeles
dc.contributor.authorLoza García, María Isabel
dc.contributor.authorSotelo Pérez, Eddy
dc.date.accessioned2020-05-24T20:18:29Z
dc.date.available2020-05-24T20:18:29Z
dc.date.issued2017
dc.identifier.citationAzuaje, 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.urihttp://hdl.handle.net/10347/22518
dc.description.abstractSome 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.sponsorshipThis 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.isoeng
dc.publisherNature 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.urihttps://creativecommons.org/licenses/by/4.0/
dc.titleDevelopment of fluorescent probes that target serotonin 5-HT2B receptors
dc.typejournal article
dc.identifier.doi10.1038/s41598-017-11370-2
dc.relation.publisherversionhttps://doi.org/10.1038/s41598-017-11370-2
dc.type.hasVersionVoR
dc.identifier.essn2045-2322
dc.rights.accessRightsopen access
dc.contributor.affiliationUniversidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
dc.contributor.affiliationUniversidade de Santiago de Compostela. Centro de Investigación en Química Biolóxica e Materiais Moleculares
dc.contributor.affiliationUniversidade de Santiago de Compostela. Departamento de Química Orgánica
dc.description.peerreviewedSI


Ficheiros no ítem

application/pdf
Nome: 2017_scirep_azuaje_development.pdf
Tamaño: 3.691 Mb
Formato: PDF


Thumbnail

Este ítem aparece na(s) seguinte(s) colección(s)

Mostrar o rexistro simple do ítem

© 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/
A licenza do ítem descríbese como
 © 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/





Recolectores:Enlaces de interese:
Universidade de Santiago de Compostela | Teléfonos: +34 881 811 000 e +34 982 820 000 | Contacto | Suxestións