The Use of Flavylium Salts as Dynamic Inhibitor Moieties for Human Cb5R

Detalhes bibliográficos
Autor(a) principal: Martínez-Costa, Oscar H.
Data de Publicação: 2023
Outros Autores: Rodrigues-Miranda, Laura, Clemente, Sofia M., Parola, António Jorge, Basílio, Nuno, Samhan-Arias, Alejandro K.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10362/150808
Resumo: Authors would like to acknowledge the Biochemistry Department in the Faculty of Medicine at the Universidad Autónoma de Madrid for the equipment and support for some of the required reagent purchases. FCT/MCTES is also acknowledged for supporting the National Portuguese NMR Network (ROTEIRO/0031/2013-PINFRA/22161/2016, co-financed by FEDER through COMPETE 2020, POCI, PORL. We thank José Paulo da Silva for the HRMS-ESI analysis. Publisher Copyright: © 2022 by the authors.
id RCAP_823de68d55bf534b51b311bd784df611
oai_identifier_str oai:run.unl.pt:10362/150808
network_acronym_str RCAP
network_name_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository_id_str 7160
spelling The Use of Flavylium Salts as Dynamic Inhibitor Moieties for Human Cb5Rchalconescytochrome b reductaseflavonoidsflavyliumhemiketalquinoidal baseAnalytical ChemistryChemistry (miscellaneous)Molecular MedicinePharmaceutical ScienceDrug DiscoveryPhysical and Theoretical ChemistryOrganic ChemistryAuthors would like to acknowledge the Biochemistry Department in the Faculty of Medicine at the Universidad Autónoma de Madrid for the equipment and support for some of the required reagent purchases. FCT/MCTES is also acknowledged for supporting the National Portuguese NMR Network (ROTEIRO/0031/2013-PINFRA/22161/2016, co-financed by FEDER through COMPETE 2020, POCI, PORL. We thank José Paulo da Silva for the HRMS-ESI analysis. Publisher Copyright: © 2022 by the authors.Cytochrome b5 reductase (Cb5R) is a flavoprotein that participates in the reduction of multiple biological redox partners. Co-localization of this protein with nitric oxide sources has been observed in neurons. In addition, the generation of superoxide anion radical by Cb5R has been observed. A search for specific inhibitors of Cb5R to understand the role of this protein in these new functions has been initiated. Previous studies have shown the ability of different flavonoids to inhibit Cb5R. Anthocyanins are a subgroup of flavonoids responsible for most red and blue colors found in flowers and fruits. Although usually represented by the flavylium cation form, these species are only stable at rather acidic pH values (pH ≤ 1). At higher pH values, the flavylium cation is involved in a dynamic reaction network comprising different neutral species with the potential ability to inhibit the activities of Cb5R. This study aims to provide insights into the molecular mechanism of interaction between flavonoids and Cb5R using flavylium salts as dynamic inhibitors. The outcome of this study might lead to the design of improved specific enzyme inhibitors in the future.DQ - Departamento de QuímicaLAQV@REQUIMTERUNMartínez-Costa, Oscar H.Rodrigues-Miranda, LauraClemente, Sofia M.Parola, António JorgeBasílio, NunoSamhan-Arias, Alejandro K.2023-03-17T22:32:22Z2023-012023-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article15application/pdfhttp://hdl.handle.net/10362/150808eng1420-3049PURE: 56248562https://doi.org/10.3390/molecules28010123info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2024-03-11T05:33:15Zoai:run.unl.pt:10362/150808Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T03:54:20.120161Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv The Use of Flavylium Salts as Dynamic Inhibitor Moieties for Human Cb5R
title The Use of Flavylium Salts as Dynamic Inhibitor Moieties for Human Cb5R
spellingShingle The Use of Flavylium Salts as Dynamic Inhibitor Moieties for Human Cb5R
Martínez-Costa, Oscar H.
chalcones
cytochrome b reductase
flavonoids
flavylium
hemiketal
quinoidal base
Analytical Chemistry
Chemistry (miscellaneous)
Molecular Medicine
Pharmaceutical Science
Drug Discovery
Physical and Theoretical Chemistry
Organic Chemistry
title_short The Use of Flavylium Salts as Dynamic Inhibitor Moieties for Human Cb5R
title_full The Use of Flavylium Salts as Dynamic Inhibitor Moieties for Human Cb5R
title_fullStr The Use of Flavylium Salts as Dynamic Inhibitor Moieties for Human Cb5R
title_full_unstemmed The Use of Flavylium Salts as Dynamic Inhibitor Moieties for Human Cb5R
title_sort The Use of Flavylium Salts as Dynamic Inhibitor Moieties for Human Cb5R
author Martínez-Costa, Oscar H.
author_facet Martínez-Costa, Oscar H.
Rodrigues-Miranda, Laura
Clemente, Sofia M.
Parola, António Jorge
Basílio, Nuno
Samhan-Arias, Alejandro K.
author_role author
author2 Rodrigues-Miranda, Laura
Clemente, Sofia M.
Parola, António Jorge
Basílio, Nuno
Samhan-Arias, Alejandro K.
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv DQ - Departamento de Química
LAQV@REQUIMTE
RUN
dc.contributor.author.fl_str_mv Martínez-Costa, Oscar H.
Rodrigues-Miranda, Laura
Clemente, Sofia M.
Parola, António Jorge
Basílio, Nuno
Samhan-Arias, Alejandro K.
dc.subject.por.fl_str_mv chalcones
cytochrome b reductase
flavonoids
flavylium
hemiketal
quinoidal base
Analytical Chemistry
Chemistry (miscellaneous)
Molecular Medicine
Pharmaceutical Science
Drug Discovery
Physical and Theoretical Chemistry
Organic Chemistry
topic chalcones
cytochrome b reductase
flavonoids
flavylium
hemiketal
quinoidal base
Analytical Chemistry
Chemistry (miscellaneous)
Molecular Medicine
Pharmaceutical Science
Drug Discovery
Physical and Theoretical Chemistry
Organic Chemistry
description Authors would like to acknowledge the Biochemistry Department in the Faculty of Medicine at the Universidad Autónoma de Madrid for the equipment and support for some of the required reagent purchases. FCT/MCTES is also acknowledged for supporting the National Portuguese NMR Network (ROTEIRO/0031/2013-PINFRA/22161/2016, co-financed by FEDER through COMPETE 2020, POCI, PORL. We thank José Paulo da Silva for the HRMS-ESI analysis. Publisher Copyright: © 2022 by the authors.
publishDate 2023
dc.date.none.fl_str_mv 2023-03-17T22:32:22Z
2023-01
2023-01-01T00:00:00Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10362/150808
url http://hdl.handle.net/10362/150808
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 1420-3049
PURE: 56248562
https://doi.org/10.3390/molecules28010123
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 15
application/pdf
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str RCAAP
institution RCAAP
reponame_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
repository.mail.fl_str_mv
_version_ 1799138132435664896

Registros relacionados