Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.

GPR55 is an orphan G-protein coupled receptor involved in various pathophysiological conditions. However, there are only a few noncannabinoid GPR55 ligands reported so far. The lack of potent and selective GPR55 ligands precludes a deep exploration of this receptor. The studies presented here focuse...

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Detalhes bibliográficos
Autores: Figuerola Asencio, Laura, Morales, Paula, Zhao, Pingwei, Hurst, Dow P, Sayed, Sommayah S, Colón, Katsuya L, Gómez Cañas, María, Fernández Ruiz, José Javier, Croatt, Mitchell P, Reggio, Patricia H, Abood, Mary E, Jagerovic, Nadine
Formato: artículo
Fecha de publicación:2023
País:España
Recursos:Universidad Complutense de Madrid (UCM)
Repositorio:Docta Complutense
Idioma:inglés
OAI Identifier:oai:docta.ucm.es:20.500.14352/133311
Acesso em linha:https://hdl.handle.net/20.500.14352/133311
Access Level:acceso abierto
Palavra-chave:GPR55
Antagonist
Cannabinoid
Thienopyrimidine
SAR
Ciencias Biomédicas
Farmacología (Medicina)
24 Ciencias de la Vida
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spelling Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.Figuerola Asencio, LauraMorales, PaulaZhao, PingweiHurst, Dow PSayed, Sommayah SColón, Katsuya LGómez Cañas, MaríaFernández Ruiz, José JavierCroatt, Mitchell PReggio, Patricia HAbood, Mary EJagerovic, NadineGPR55AntagonistCannabinoidThienopyrimidineSARCiencias BiomédicasFarmacología (Medicina)24 Ciencias de la VidaGPR55 is an orphan G-protein coupled receptor involved in various pathophysiological conditions. However, there are only a few noncannabinoid GPR55 ligands reported so far. The lack of potent and selective GPR55 ligands precludes a deep exploration of this receptor. The studies presented here focused on a thienopyrimidine scaffold based on the GPR55 antagonist ML192, previously discovered by high-throughput screening. The GPR55 activities of the new synthesized compounds were assessed using β-arrestin recruitment assays in Chinese hamster ovary cells overexpressing human GPR55. Some derivatives were identified as GPR55 antagonists with functional efficacy and selectivity versus CB1 and CB2 cannabinoid receptors.American Chemical Society publicationsUniversidad Complutense de Madrid20232023-01-0120232023-01-01journal articlehttp://purl.org/coar/resource_type/c_6501VoRhttp://purl.org/coar/version/c_970fb48d4fbd8a85info:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/20.500.14352/133311reponame:Docta Complutenseinstname:Universidad Complutense de Madrid (UCM)Inglésengopen accesshttp://purl.org/coar/access_right/c_abf2Attribution-NonCommercial-NoDerivatives 4.0 Internationalhttp://creativecommons.org/licenses/by-nc-nd/4.0/info:eu-repo/semantics/openAccessoai:docta.ucm.es:20.500.14352/1333112026-06-02T12:44:21Z
dc.title.none.fl_str_mv Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
title Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
spellingShingle Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
Figuerola Asencio, Laura
GPR55
Antagonist
Cannabinoid
Thienopyrimidine
SAR
Ciencias Biomédicas
Farmacología (Medicina)
24 Ciencias de la Vida
title_short Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
title_full Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
title_fullStr Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
title_full_unstemmed Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
title_sort Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
dc.creator.none.fl_str_mv Figuerola Asencio, Laura
Morales, Paula
Zhao, Pingwei
Hurst, Dow P
Sayed, Sommayah S
Colón, Katsuya L
Gómez Cañas, María
Fernández Ruiz, José Javier
Croatt, Mitchell P
Reggio, Patricia H
Abood, Mary E
Jagerovic, Nadine
author Figuerola Asencio, Laura
author_facet Figuerola Asencio, Laura
Morales, Paula
Zhao, Pingwei
Hurst, Dow P
Sayed, Sommayah S
Colón, Katsuya L
Gómez Cañas, María
Fernández Ruiz, José Javier
Croatt, Mitchell P
Reggio, Patricia H
Abood, Mary E
Jagerovic, Nadine
author_role author
author2 Morales, Paula
Zhao, Pingwei
Hurst, Dow P
Sayed, Sommayah S
Colón, Katsuya L
Gómez Cañas, María
Fernández Ruiz, José Javier
Croatt, Mitchell P
Reggio, Patricia H
Abood, Mary E
Jagerovic, Nadine
author2_role author
author
author
author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Universidad Complutense de Madrid
dc.subject.none.fl_str_mv GPR55
Antagonist
Cannabinoid
Thienopyrimidine
SAR
Ciencias Biomédicas
Farmacología (Medicina)
24 Ciencias de la Vida
topic GPR55
Antagonist
Cannabinoid
Thienopyrimidine
SAR
Ciencias Biomédicas
Farmacología (Medicina)
24 Ciencias de la Vida
description GPR55 is an orphan G-protein coupled receptor involved in various pathophysiological conditions. However, there are only a few noncannabinoid GPR55 ligands reported so far. The lack of potent and selective GPR55 ligands precludes a deep exploration of this receptor. The studies presented here focused on a thienopyrimidine scaffold based on the GPR55 antagonist ML192, previously discovered by high-throughput screening. The GPR55 activities of the new synthesized compounds were assessed using β-arrestin recruitment assays in Chinese hamster ovary cells overexpressing human GPR55. Some derivatives were identified as GPR55 antagonists with functional efficacy and selectivity versus CB1 and CB2 cannabinoid receptors.
publishDate 2023
dc.date.none.fl_str_mv 2023
2023-01-01
2023
2023-01-01
dc.type.none.fl_str_mv journal article
http://purl.org/coar/resource_type/c_6501
VoR
http://purl.org/coar/version/c_970fb48d4fbd8a85
dc.type.openaire.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv https://hdl.handle.net/20.500.14352/133311
url https://hdl.handle.net/20.500.14352/133311
dc.language.none.fl_str_mv Inglés
eng
language_invalid_str_mv Inglés
language eng
dc.rights.none.fl_str_mv open access
http://purl.org/coar/access_right/c_abf2
Attribution-NonCommercial-NoDerivatives 4.0 International
http://creativecommons.org/licenses/by-nc-nd/4.0/
dc.rights.openaire.fl_str_mv info:eu-repo/semantics/openAccess
rights_invalid_str_mv open access
http://purl.org/coar/access_right/c_abf2
Attribution-NonCommercial-NoDerivatives 4.0 International
http://creativecommons.org/licenses/by-nc-nd/4.0/
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv American Chemical Society publications
publisher.none.fl_str_mv American Chemical Society publications
dc.source.none.fl_str_mv reponame:Docta Complutense
instname:Universidad Complutense de Madrid (UCM)
instname_str Universidad Complutense de Madrid (UCM)
reponame_str Docta Complutense
collection Docta Complutense
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,811543

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