A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery

The identification of new modulators for Cannabinoid Receptors (CBRs) has garnered significant attention in drug discovery over recent years, owing to their manifold pathophysiological implications. In the context of hit identification, the availability of robust and sensitive high-throughput screen...

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Detalles Bibliográficos
Autores: Navarro, G., Sotelo, E., Raïch, I., Loza García, María Isabel, Brea Floriani, José Manuel, Majellaro, M.
Tipo de recurso: artículo
Fecha de publicación:2023
País:España
Institución:Servizo Galego de Saúde (SERGAS)
Repositorio:RUNA. Repositorio da Consellería de Sanidade e Sergas
OAI Identifier:oai:runa.sergas.gal:20.500.11940/21004
Acceso en línea:https://portalcientifico.sergas.gal//documentos/65a4608d528f145c72000527
http://hdl.handle.net/20.500.11940/21004
Access Level:acceso abierto
Palabra clave:Ligands
Fluorescence Resonance Energy Transfer
Protein Binding
Receptors, Cannabinoid
Drug Discovery
Coloring Agents
AS Santiago
IDIS
id ES_b4fbfce4abbb5135631a65778f751fbf
oai_identifier_str oai:runa.sergas.gal:20.500.11940/21004
network_acronym_str ES
network_name_str España
repository_id_str
spelling A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands DiscoveryNavarro, G.Sotelo, E.Raïch, I.Loza García, María IsabelBrea Floriani, José ManuelMajellaro, M.LigandsFluorescence Resonance Energy TransferProtein BindingReceptors, CannabinoidDrug DiscoveryColoring AgentsAS SantiagoIDISThe identification of new modulators for Cannabinoid Receptors (CBRs) has garnered significant attention in drug discovery over recent years, owing to their manifold pathophysiological implications. In the context of hit identification, the availability of robust and sensitive high-throughput screening assays is essential to enhance the likelihood of success. In this study, we present the development and validation of a Tag-lite® binding assay designed for screening hCB1/hCB2 binding, employing a dual fluorescent ligand, CELT-335. Representative ligands for CBRs, exhibiting diverse affinity and functional profiles, were utilized as reference compounds to validate the robustness and efficiency of the newly developed Tag-lite® binding assay protocol. The homogeneous format, coupled with the sensitivity and optimal performance of the fluorescent ligand CELT-335, establishes this assay as a viable and reliable method for screening in hit and lead identification campaigns.We thank Revvity, Codolet (France) for providing biological material for the HTRF Tag-lite (R) validation in CB2R and COST Action CA18133/European Research Network on Signal Transduction (ERNEST) for support and networking among the different groups involved in this work.2023info:eu-repo/semantics/articlehttps://portalcientifico.sergas.gal//documentos/65a4608d528f145c72000527http://hdl.handle.net/20.500.11940/21004reponame:RUNA. Repositorio da Consellería de Sanidade e Sergasinstname:Servizo Galego de Saúde (SERGAS)Ingléshttp://creativecommons.org/licenses/by/4.0/info:eu-repo/semantics/openAccessoai:runa.sergas.gal:20.500.11940/210042026-06-12T08:40:47Z
dc.title.none.fl_str_mv A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery
title A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery
spellingShingle A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery
Navarro, G.
Ligands
Fluorescence Resonance Energy Transfer
Protein Binding
Receptors, Cannabinoid
Drug Discovery
Coloring Agents
AS Santiago
IDIS
title_short A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery
title_full A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery
title_fullStr A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery
title_full_unstemmed A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery
title_sort A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery
dc.creator.none.fl_str_mv Navarro, G.
Sotelo, E.
Raïch, I.
Loza García, María Isabel
Brea Floriani, José Manuel
Majellaro, M.
author Navarro, G.
author_facet Navarro, G.
Sotelo, E.
Raïch, I.
Loza García, María Isabel
Brea Floriani, José Manuel
Majellaro, M.
author_role author
author2 Sotelo, E.
Raïch, I.
Loza García, María Isabel
Brea Floriani, José Manuel
Majellaro, M.
author2_role author
author
author
author
author
dc.subject.none.fl_str_mv Ligands
Fluorescence Resonance Energy Transfer
Protein Binding
Receptors, Cannabinoid
Drug Discovery
Coloring Agents
AS Santiago
IDIS
topic Ligands
Fluorescence Resonance Energy Transfer
Protein Binding
Receptors, Cannabinoid
Drug Discovery
Coloring Agents
AS Santiago
IDIS
description The identification of new modulators for Cannabinoid Receptors (CBRs) has garnered significant attention in drug discovery over recent years, owing to their manifold pathophysiological implications. In the context of hit identification, the availability of robust and sensitive high-throughput screening assays is essential to enhance the likelihood of success. In this study, we present the development and validation of a Tag-lite® binding assay designed for screening hCB1/hCB2 binding, employing a dual fluorescent ligand, CELT-335. Representative ligands for CBRs, exhibiting diverse affinity and functional profiles, were utilized as reference compounds to validate the robustness and efficiency of the newly developed Tag-lite® binding assay protocol. The homogeneous format, coupled with the sensitivity and optimal performance of the fluorescent ligand CELT-335, establishes this assay as a viable and reliable method for screening in hit and lead identification campaigns.
publishDate 2023
dc.date.none.fl_str_mv 2023
dc.type.none.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv https://portalcientifico.sergas.gal//documentos/65a4608d528f145c72000527
http://hdl.handle.net/20.500.11940/21004
url https://portalcientifico.sergas.gal//documentos/65a4608d528f145c72000527
http://hdl.handle.net/20.500.11940/21004
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.rights.none.fl_str_mv http://creativecommons.org/licenses/by/4.0/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv http://creativecommons.org/licenses/by/4.0/
eu_rights_str_mv openAccess
dc.source.none.fl_str_mv reponame:RUNA. Repositorio da Consellería de Sanidade e Sergas
instname:Servizo Galego de Saúde (SERGAS)
instname_str Servizo Galego de Saúde (SERGAS)
reponame_str RUNA. Repositorio da Consellería de Sanidade e Sergas
collection RUNA. Repositorio da Consellería de Sanidade e Sergas
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15.811543

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