Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase

The synthesis of four tetra-tacrine clusters where the tacrine binding units are attached to a central scaffold via linkers of variable lengths is described. The multivalent inhibition potencies for the tacrine clusters were investigated for the inhibition of acetylcholinesterase. Two of the tacrine...

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Autores: Evangelista, Tereza Cristina Santos, López López, Óscar, Ferreira, Sabrina Baptista, Fernández-Bolaños Guzmán, José María, Sydnes, Magne O., Lindbäck, Emil
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2021
País:España
Institución:Universidad de Sevilla (US)
Repositorio:idUS. Depósito de Investigación de la Universidad de Sevilla
OAI Identifier:oai:idus.us.es:11441/131938
Acceso en línea:https://hdl.handle.net/11441/131938
https://doi.org/10.1080/14756366.2021.1954917
Access Level:acceso abierto
Palabra clave:Acetylcholinesterase
CuAAC
multivalent interactions
multivalent inhibition potency
tacrine
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network_acronym_str ES
network_name_str España
repository_id_str
spelling Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesteraseEvangelista, Tereza Cristina SantosLópez López, ÓscarFerreira, Sabrina BaptistaFernández-Bolaños Guzmán, José MaríaSydnes, Magne O.Lindbäck, EmilAcetylcholinesteraseCuAACmultivalent interactionsmultivalent inhibition potencytacrineThe synthesis of four tetra-tacrine clusters where the tacrine binding units are attached to a central scaffold via linkers of variable lengths is described. The multivalent inhibition potencies for the tacrine clusters were investigated for the inhibition of acetylcholinesterase. Two of the tacrine clusters displayed a small but significant multivalent inhibition potency in which the binding affinity of each of the tacrine binding units increased up to 3.2 times when they are connected to the central scaffold.Junta de Andalucía. FQM134Ministerio de Ciencia e Innovación de España (MICINN) y fondos FEDER de la Unión Europea. CTQ2016-78703-PTaylor & Francis Open AccessElectrónica y ElectromagnetismoFQM134: Química Fina de CarbohidratosJunta de AndalucíaUniversidad de Stavanger. NoruegaMinisterio de Ciencia e Innovación (MICIN). EspañaEuropean Commission (EC). Fondo Europeo de Desarrollo Regional (FEDER)2021info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfapplication/pdfhttps://hdl.handle.net/11441/131938https://doi.org/10.1080/14756366.2021.1954917reponame:idUS. Depósito de Investigación de la Universidad de Sevillainstname:Universidad de Sevilla (US)InglésJournal of Enzyme Inhibition and Medicinal Chemistry, 36 (1), 1659-1664.FQM134CTQ2016-78703-Phttps://doi.org/10.1080/14756366.2021.1954917info:eu-repo/semantics/openAccessoai:idus.us.es:11441/1319382026-06-17T12:51:07Z
dc.title.none.fl_str_mv Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase
title Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase
spellingShingle Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase
Evangelista, Tereza Cristina Santos
Acetylcholinesterase
CuAAC
multivalent interactions
multivalent inhibition potency
tacrine
title_short Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase
title_full Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase
title_fullStr Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase
title_full_unstemmed Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase
title_sort Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase
dc.creator.none.fl_str_mv Evangelista, Tereza Cristina Santos
López López, Óscar
Ferreira, Sabrina Baptista
Fernández-Bolaños Guzmán, José María
Sydnes, Magne O.
Lindbäck, Emil
author Evangelista, Tereza Cristina Santos
author_facet Evangelista, Tereza Cristina Santos
López López, Óscar
Ferreira, Sabrina Baptista
Fernández-Bolaños Guzmán, José María
Sydnes, Magne O.
Lindbäck, Emil
author_role author
author2 López López, Óscar
Ferreira, Sabrina Baptista
Fernández-Bolaños Guzmán, José María
Sydnes, Magne O.
Lindbäck, Emil
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv Electrónica y Electromagnetismo
FQM134: Química Fina de Carbohidratos
Junta de Andalucía
Universidad de Stavanger. Noruega
Ministerio de Ciencia e Innovación (MICIN). España
European Commission (EC). Fondo Europeo de Desarrollo Regional (FEDER)
dc.subject.none.fl_str_mv Acetylcholinesterase
CuAAC
multivalent interactions
multivalent inhibition potency
tacrine
topic Acetylcholinesterase
CuAAC
multivalent interactions
multivalent inhibition potency
tacrine
description The synthesis of four tetra-tacrine clusters where the tacrine binding units are attached to a central scaffold via linkers of variable lengths is described. The multivalent inhibition potencies for the tacrine clusters were investigated for the inhibition of acetylcholinesterase. Two of the tacrine clusters displayed a small but significant multivalent inhibition potency in which the binding affinity of each of the tacrine binding units increased up to 3.2 times when they are connected to the central scaffold.
publishDate 2021
dc.date.none.fl_str_mv 2021
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/11441/131938
https://doi.org/10.1080/14756366.2021.1954917
url https://hdl.handle.net/11441/131938
https://doi.org/10.1080/14756366.2021.1954917
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Journal of Enzyme Inhibition and Medicinal Chemistry, 36 (1), 1659-1664.
FQM134
CTQ2016-78703-P
https://doi.org/10.1080/14756366.2021.1954917
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Taylor & Francis Open Access
publisher.none.fl_str_mv Taylor & Francis Open Access
dc.source.none.fl_str_mv reponame:idUS. Depósito de Investigación de la Universidad de Sevilla
instname:Universidad de Sevilla (US)
instname_str Universidad de Sevilla (US)
reponame_str idUS. Depósito de Investigación de la Universidad de Sevilla
collection idUS. Depósito de Investigación de la Universidad de Sevilla
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,301603

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