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
.jpg)
- Institución
- Universidad Nacional de La Plata
- OAI Identificador
- oai:sedici.unlp.edu.ar:10915/103425
Ver los metadatos del registro completo
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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:UNLP2025-10-15T11:14:24Zoai: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:13292025-10-15 11:14:24.594SEDICI (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. |
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2017 |
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2017 |
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eng |
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