A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells

Class B G protein-coupled receptors (GPCRs) are involved in a variety of human pathophysiological states. These groups of membrane receptors are less studied than class A GPCRs due to the lack of structural information, delayed small molecule drug discovery, and scarce fluorescence detection tools a...

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Autores: Szalai, Alan Marcelo, Armando, Natalia Giannina, Barabas, Federico Martín, Stefani, Fernando Daniel, Giordano, Luciana, Bari, Sara Elizabeth, Cavasotto, Claudio Norberto, Silberstein Cuña, Susana Iris, Aramendia, Pedro Francisco
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2018
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/91269
Acceso en línea:http://hdl.handle.net/11336/91269
Access Level:acceso abierto
Palabra clave:aza-BODIPY
Super-resolution
CRH receptor
hippocampal neurons
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
id AR_79ce501dfaa700dcc0a6515237bbbc02
oai_identifier_str oai:ri.conicet.gov.ar:11336/91269
network_acronym_str AR
network_name_str Argentina
repository_id_str
dc.title.none.fl_str_mv A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells
title A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells
spellingShingle A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells
Szalai, Alan Marcelo
aza-BODIPY
Super-resolution
CRH receptor
hippocampal neurons
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
title_short A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells
title_full A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells
title_fullStr A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells
title_full_unstemmed A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells
title_sort A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells
dc.creator.none.fl_str_mv Szalai, Alan Marcelo
Armando, Natalia Giannina
Barabas, Federico Martín
Stefani, Fernando Daniel
Giordano, Luciana
Bari, Sara Elizabeth
Cavasotto, Claudio Norberto
Silberstein Cuña, Susana Iris
Aramendia, Pedro Francisco
author Szalai, Alan Marcelo
author_facet Szalai, Alan Marcelo
Armando, Natalia Giannina
Barabas, Federico Martín
Stefani, Fernando Daniel
Giordano, Luciana
Bari, Sara Elizabeth
Cavasotto, Claudio Norberto
Silberstein Cuña, Susana Iris
Aramendia, Pedro Francisco
author_role author
author2 Armando, Natalia Giannina
Barabas, Federico Martín
Stefani, Fernando Daniel
Giordano, Luciana
Bari, Sara Elizabeth
Cavasotto, Claudio Norberto
Silberstein Cuña, Susana Iris
Aramendia, Pedro Francisco
author2_role author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv aza-BODIPY
Super-resolution
CRH receptor
hippocampal neurons
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
topic aza-BODIPY
Super-resolution
CRH receptor
hippocampal neurons
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
description Class B G protein-coupled receptors (GPCRs) are involved in a variety of human pathophysiological states. These groups of membrane receptors are less studied than class A GPCRs due to the lack of structural information, delayed small molecule drug discovery, and scarce fluorescence detection tools available. The class B corticotropin-releasing hormone type 1 receptor (CRHR1) is a key player in the stress response whose dysregulation is critically involved in stress-related disorders: psychiatric conditions (i.e. depression, anxiety, and addictions), neuroendocrinological alterations, and neurodegenerative diseases. Here, we present a strategy to label GPCRs with a small fluorescent antagonist that permits the observation of the receptor in live cells through stochastic optical reconstruction microscopy (STORM) with 23 nm resolution. The marker, an aza-BODIPY derivative, was designed based on computational docking studies, then synthesized, and finally tested in biological cells. Experiments on hippocampal neurons demonstrate antagonist effects in similar concentrations as the well-established antagonist CP-376395. A quantitative analysis of two color STORM images enabled the determination of the binding affinity of the new marker in the cellular environment.
publishDate 2018
dc.date.none.fl_str_mv 2018-11
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/91269
Szalai, Alan Marcelo; Armando, Natalia Giannina; Barabas, Federico Martín; Stefani, Fernando Daniel; Giordano, Luciana; et al.; A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells; Royal Society of Chemistry; Physical Chemistry Chemical Physics; 20; 46; 11-2018; 29212-29220
1463-9076
CONICET Digital
CONICET
url http://hdl.handle.net/11336/91269
identifier_str_mv Szalai, Alan Marcelo; Armando, Natalia Giannina; Barabas, Federico Martín; Stefani, Fernando Daniel; Giordano, Luciana; et al.; A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells; Royal Society of Chemistry; Physical Chemistry Chemical Physics; 20; 46; 11-2018; 29212-29220
1463-9076
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1039/C8CP06196C
info:eu-repo/semantics/altIdentifier/url/https://pubs.rsc.org/en/content/articlelanding/2018/CP/C8CP06196C
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Royal Society of Chemistry
publisher.none.fl_str_mv Royal Society of Chemistry
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
_version_ 1799195662918615040
spelling A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cellsSzalai, Alan MarceloArmando, Natalia GianninaBarabas, Federico MartínStefani, Fernando DanielGiordano, LucianaBari, Sara ElizabethCavasotto, Claudio NorbertoSilberstein Cuña, Susana IrisAramendia, Pedro Franciscoaza-BODIPYSuper-resolutionCRH receptorhippocampal neuronshttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1Class B G protein-coupled receptors (GPCRs) are involved in a variety of human pathophysiological states. These groups of membrane receptors are less studied than class A GPCRs due to the lack of structural information, delayed small molecule drug discovery, and scarce fluorescence detection tools available. The class B corticotropin-releasing hormone type 1 receptor (CRHR1) is a key player in the stress response whose dysregulation is critically involved in stress-related disorders: psychiatric conditions (i.e. depression, anxiety, and addictions), neuroendocrinological alterations, and neurodegenerative diseases. Here, we present a strategy to label GPCRs with a small fluorescent antagonist that permits the observation of the receptor in live cells through stochastic optical reconstruction microscopy (STORM) with 23 nm resolution. The marker, an aza-BODIPY derivative, was designed based on computational docking studies, then synthesized, and finally tested in biological cells. Experiments on hippocampal neurons demonstrate antagonist effects in similar concentrations as the well-established antagonist CP-376395. A quantitative analysis of two color STORM images enabled the determination of the binding affinity of the new marker in the cellular environment.Fil: Szalai, Alan Marcelo. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Centro de Investigaciones en Bionanociencias "Elizabeth Jares Erijman"; ArgentinaFil: Armando, Natalia Giannina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Instituto de Investigación en Biomedicina de Buenos Aires - Instituto Partner de la Sociedad Max Planck; ArgentinaFil: Barabas, Federico Martín. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Centro de Investigaciones en Bionanociencias "Elizabeth Jares Erijman"; ArgentinaFil: Stefani, Fernando Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Centro de Investigaciones en Bionanociencias "Elizabeth Jares Erijman"; ArgentinaFil: Giordano, Luciana. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Centro de Investigaciones en Bionanociencias "Elizabeth Jares Erijman"; ArgentinaFil: Bari, Sara Elizabeth. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Instituto de Química, Física de los Materiales, Medioambiente y Energía. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Instituto de Química, Física de los Materiales, Medioambiente y Energía; ArgentinaFil: Cavasotto, Claudio Norberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Instituto de Investigación en Biomedicina de Buenos Aires - Instituto Partner de la Sociedad Max Planck; ArgentinaFil: Silberstein Cuña, Susana Iris. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Instituto de Investigación en Biomedicina de Buenos Aires - Instituto Partner de la Sociedad Max Planck; ArgentinaFil: Aramendia, Pedro Francisco. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Centro de Investigaciones en Bionanociencias "Elizabeth Jares Erijman"; ArgentinaRoyal Society of Chemistry2018-11info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/91269Szalai, Alan Marcelo; Armando, Natalia Giannina; Barabas, Federico Martín; Stefani, Fernando Daniel; Giordano, Luciana; et al.; A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells; Royal Society of Chemistry; Physical Chemistry Chemical Physics; 20; 46; 11-2018; 29212-292201463-9076CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1039/C8CP06196Cinfo:eu-repo/semantics/altIdentifier/url/https://pubs.rsc.org/en/content/articlelanding/2018/CP/C8CP06196Cinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2024-05-08T13:59:34Zoai:ri.conicet.gov.ar:11336/91269instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982024-05-08 13:59:34.641CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
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