Kinase Inhibitors with Antiepileptic Properties Identified with a Novel in Vitro Screening Platform.
Int J Mol Sci
; 20(10)2019 May 21.
Article
em En
| MEDLINE
| ID: mdl-31117204
Kinase signaling plays an important role in acquired epilepsy, but only a small percentage of the total kinome has been investigated in this context. A major roadblock that prevents the systematic investigation of the contributions of kinase signaling networks is the slow speed of experiments designed to test the chronic effects of target inhibition in epilepsy models. We developed a novel in vitro screening platform based on microwire recordings from an organotypic hippocampal culture model of acquired epilepsy. This platform enables the direct, parallel determination of the effects of compounds on spontaneous epileptiform activity. The platform also enables repeated recordings from the same culture over two-week long experiments. We screened 45 kinase inhibitors and quantified their effects on seizure duration, the frequency of paroxysmal activity, and electrographic load. We identified several inhibitors with previously unknown antiepileptic properties. We also used kinase inhibition profile cross-referencing to identify kinases that are inhibited by seizure-suppressing compounds, but not by compounds that had no effect on seizures.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Técnicas de Cultura de Órgãos
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Inibidores de Proteínas Quinases
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Avaliação Pré-Clínica de Medicamentos
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Epilepsia
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Hipocampo
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Anticonvulsivantes
Tipo de estudo:
Diagnostic_studies
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Screening_studies
Limite:
Animals
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article