Computer-Aided Recognition of ABC Transporters Substrates and Its Application to the Development of New Drugs for Refractory Epilepsy
| Autor: | Andrea Enrique, Pablo Hernán Palestro, Guido Pesce, Alan Talevi, Manuel Couyoupetrou, María Esperanza Ruiz, Luis E. Bruno-Blanch, Luciana Gavernet, Melisa Edith Gantner, Mauricio E. Di Ianni |
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| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Drug Drug Resistant Epilepsy Abcg2 media_common.quotation_subject ABCG2 Antiepileptic drugs ATP-binding cassette transporter Pharmacology P-glycoprotein Bioinformatics 03 medical and health sciences Epilepsy 0302 clinical medicine medicine Animals Humans Refractory epilepsy media_common Transporter hypothesis biology Drug discovery business.industry Transporter ABCB1 General Medicine Química medicine.disease Farmacia Breast cancer resistance protein 030104 developmental biology ABC transporters biology.protein Computer-Aided Design ATP-Binding Cassette Transporters business 030217 neurology & neurosurgery |
| Zdroj: | SEDICI (UNLP) Universidad Nacional de La Plata instacron:UNLP |
| Popis: | 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 |
| Databáze: | OpenAIRE |
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