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

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 s...

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Autores principales: 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
Formato: Articulo
Lenguaje:Inglés
Publicado: 2017
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Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/103425
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id I19-R120-10915-103425
record_format dspace
institution Universidad Nacional de La Plata
institution_str I-19
repository_str R-120
collection SEDICI (UNLP)
language Inglés
topic Farmacia
Química
ABC transporters
ABCB1
ABCG2
Antiepileptic drugs
Breast cancer resistance protein
Drug discovery
P-glycoprotein
Refractory epilepsy
Transporter hypothesis
spellingShingle Farmacia
Química
ABC transporters
ABCB1
ABCG2
Antiepileptic drugs
Breast cancer resistance protein
Drug discovery
P-glycoprotein
Refractory epilepsy
Transporter hypothesis
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
Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy
topic_facet Farmacia
Química
ABC transporters
ABCB1
ABCG2
Antiepileptic drugs
Breast cancer resistance protein
Drug discovery
P-glycoprotein
Refractory epilepsy
Transporter hypothesis
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.
format Articulo
Articulo
author 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_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_sort Couyoupetrou, Manuel
title Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy
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
publishDate 2017
url http://sedici.unlp.edu.ar/handle/10915/103425
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