Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy

Autores
Couyoupetrou, Manuel; Gantner, Melisa Edith; Di Ianni, Mauricio Emiliano; Palestro, Pablo Hernán; Enrique, Andrea Verónica; Gavernet, Luciana; Ruiz, María Esperanza; Pesce, Guido; Bruno Blanch, Luis Enrique; Talevi, Alan
Año de publicación
2017
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Despite the introduction of more than 15 third generation antiepileptic drugs to the market from 1990 to the moment, about one third of the epileptic patients still suffer from refractory to intractable epilepsy. Several hypotheses seek to explain the failure of drug treatments to control epilepsy symptoms in such patients. The most studied one proposes that drug resistance might be related with regional overactivity of efflux transporters from the ATP-Binding Cassette (ABC) superfamily at the blood-brain barrier and/or the epileptic foci in the brain. Different strategies have been conceived to address the transporter hypothesis, among them inhibiting or down-regulating the efflux transporters or bypassing them through a diversity of artifices. Here, we review scientific evidence supporting the transporter hypothesis along with its limitations, as well as computer-assisted early recognition of ABC transporter substrates as an interesting strategy to develop novel antiepileptic drugs capable of treating refractory epilepsy linked to ABC transporters overactivity.
Laboratorio de Investigación y Desarrollo de Bioactivos
Materia
Farmacia
Química
ABC transporters
ABCB1
ABCG2
Antiepileptic drugs
Breast cancer resistance protein
Drug discovery
P-glycoprotein
Refractory epilepsy
Transporter hypothesis
Nivel de accesibilidad
acceso abierto
Condiciones de uso
http://creativecommons.org/licenses/by-nc-sa/4.0/
Repositorio
SEDICI (UNLP)
Institución
Universidad Nacional de La Plata
OAI Identificador
oai:sedici.unlp.edu.ar:10915/103425

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network_name_str SEDICI (UNLP)
spelling Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory EpilepsyCouyoupetrou, ManuelGantner, Melisa EdithDi Ianni, Mauricio EmilianoPalestro, Pablo HernánEnrique, Andrea VerónicaGavernet, LucianaRuiz, María EsperanzaPesce, GuidoBruno Blanch, Luis EnriqueTalevi, AlanFarmaciaQuímicaABC transportersABCB1ABCG2Antiepileptic drugsBreast cancer resistance proteinDrug discoveryP-glycoproteinRefractory epilepsyTransporter hypothesisDespite the introduction of more than 15 third generation antiepileptic drugs to the market from 1990 to the moment, about one third of the epileptic patients still suffer from refractory to intractable epilepsy. Several hypotheses seek to explain the failure of drug treatments to control epilepsy symptoms in such patients. The most studied one proposes that drug resistance might be related with regional overactivity of efflux transporters from the ATP-Binding Cassette (ABC) superfamily at the blood-brain barrier and/or the epileptic foci in the brain. Different strategies have been conceived to address the transporter hypothesis, among them inhibiting or down-regulating the efflux transporters or bypassing them through a diversity of artifices. Here, we review scientific evidence supporting the transporter hypothesis along with its limitations, as well as computer-assisted early recognition of ABC transporter substrates as an interesting strategy to develop novel antiepileptic drugs capable of treating refractory epilepsy linked to ABC transporters overactivity.Laboratorio de Investigación y Desarrollo de Bioactivos2017info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionArticulohttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdf205-215http://sedici.unlp.edu.ar/handle/10915/103425enginfo:eu-repo/semantics/altIdentifier/issn/1875-5607info:eu-repo/semantics/altIdentifier/doi/10.2174/1389557516666161013103408info:eu-repo/semantics/openAccesshttp://creativecommons.org/licenses/by-nc-sa/4.0/Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International (CC BY-NC-SA 4.0)reponame:SEDICI (UNLP)instname:Universidad Nacional de La Platainstacron:UNLP2025-09-29T11:22:28Zoai:sedici.unlp.edu.ar:10915/103425Institucionalhttp://sedici.unlp.edu.ar/Universidad públicaNo correspondehttp://sedici.unlp.edu.ar/oai/snrdalira@sedici.unlp.edu.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:13292025-09-29 11:22:28.433SEDICI (UNLP) - Universidad Nacional de La Platafalse
dc.title.none.fl_str_mv Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy
title Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy
spellingShingle Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy
Couyoupetrou, Manuel
Farmacia
Química
ABC transporters
ABCB1
ABCG2
Antiepileptic drugs
Breast cancer resistance protein
Drug discovery
P-glycoprotein
Refractory epilepsy
Transporter hypothesis
title_short Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy
title_full Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy
title_fullStr Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy
title_full_unstemmed Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy
title_sort Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy
dc.creator.none.fl_str_mv Couyoupetrou, Manuel
Gantner, Melisa Edith
Di Ianni, Mauricio Emiliano
Palestro, Pablo Hernán
Enrique, Andrea Verónica
Gavernet, Luciana
Ruiz, María Esperanza
Pesce, Guido
Bruno Blanch, Luis Enrique
Talevi, Alan
author Couyoupetrou, Manuel
author_facet Couyoupetrou, Manuel
Gantner, Melisa Edith
Di Ianni, Mauricio Emiliano
Palestro, Pablo Hernán
Enrique, Andrea Verónica
Gavernet, Luciana
Ruiz, María Esperanza
Pesce, Guido
Bruno Blanch, Luis Enrique
Talevi, Alan
author_role author
author2 Gantner, Melisa Edith
Di Ianni, Mauricio Emiliano
Palestro, Pablo Hernán
Enrique, Andrea Verónica
Gavernet, Luciana
Ruiz, María Esperanza
Pesce, Guido
Bruno Blanch, Luis Enrique
Talevi, Alan
author2_role author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Farmacia
Química
ABC transporters
ABCB1
ABCG2
Antiepileptic drugs
Breast cancer resistance protein
Drug discovery
P-glycoprotein
Refractory epilepsy
Transporter hypothesis
topic Farmacia
Química
ABC transporters
ABCB1
ABCG2
Antiepileptic drugs
Breast cancer resistance protein
Drug discovery
P-glycoprotein
Refractory epilepsy
Transporter hypothesis
dc.description.none.fl_txt_mv Despite the introduction of more than 15 third generation antiepileptic drugs to the market from 1990 to the moment, about one third of the epileptic patients still suffer from refractory to intractable epilepsy. Several hypotheses seek to explain the failure of drug treatments to control epilepsy symptoms in such patients. The most studied one proposes that drug resistance might be related with regional overactivity of efflux transporters from the ATP-Binding Cassette (ABC) superfamily at the blood-brain barrier and/or the epileptic foci in the brain. Different strategies have been conceived to address the transporter hypothesis, among them inhibiting or down-regulating the efflux transporters or bypassing them through a diversity of artifices. Here, we review scientific evidence supporting the transporter hypothesis along with its limitations, as well as computer-assisted early recognition of ABC transporter substrates as an interesting strategy to develop novel antiepileptic drugs capable of treating refractory epilepsy linked to ABC transporters overactivity.
Laboratorio de Investigación y Desarrollo de Bioactivos
description Despite the introduction of more than 15 third generation antiepileptic drugs to the market from 1990 to the moment, about one third of the epileptic patients still suffer from refractory to intractable epilepsy. Several hypotheses seek to explain the failure of drug treatments to control epilepsy symptoms in such patients. The most studied one proposes that drug resistance might be related with regional overactivity of efflux transporters from the ATP-Binding Cassette (ABC) superfamily at the blood-brain barrier and/or the epileptic foci in the brain. Different strategies have been conceived to address the transporter hypothesis, among them inhibiting or down-regulating the efflux transporters or bypassing them through a diversity of artifices. Here, we review scientific evidence supporting the transporter hypothesis along with its limitations, as well as computer-assisted early recognition of ABC transporter substrates as an interesting strategy to develop novel antiepileptic drugs capable of treating refractory epilepsy linked to ABC transporters overactivity.
publishDate 2017
dc.date.none.fl_str_mv 2017
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
Articulo
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://sedici.unlp.edu.ar/handle/10915/103425
url http://sedici.unlp.edu.ar/handle/10915/103425
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/issn/1875-5607
info:eu-repo/semantics/altIdentifier/doi/10.2174/1389557516666161013103408
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
http://creativecommons.org/licenses/by-nc-sa/4.0/
Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International (CC BY-NC-SA 4.0)
eu_rights_str_mv openAccess
rights_invalid_str_mv http://creativecommons.org/licenses/by-nc-sa/4.0/
Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International (CC BY-NC-SA 4.0)
dc.format.none.fl_str_mv application/pdf
205-215
dc.source.none.fl_str_mv reponame:SEDICI (UNLP)
instname:Universidad Nacional de La Plata
instacron:UNLP
reponame_str SEDICI (UNLP)
collection SEDICI (UNLP)
instname_str Universidad Nacional de La Plata
instacron_str UNLP
institution UNLP
repository.name.fl_str_mv SEDICI (UNLP) - Universidad Nacional de La Plata
repository.mail.fl_str_mv alira@sedici.unlp.edu.ar
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