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ACS Chem Biol ; 13(5): 1361-1369, 2018 05 18.
Artículo en Inglés | MEDLINE | ID: mdl-29671577

RESUMEN

A lack of viable hits, increasing resistance, and limited knowledge on mode of action is hindering drug discovery for many diseases. To optimize prioritization and accelerate the discovery process, a strategy to cluster compounds based on more than chemical structure is required. We show the power of metabolomics in comparing effects on metabolism of 28 different candidate treatments for Leishmaniasis (25 from the GSK Leishmania box, two analogues of Leishmania box series, and amphotericin B as a gold standard treatment), tested in the axenic amastigote form of Leishmania donovani. Capillary electrophoresis-mass spectrometry was applied to identify the metabolic profile of Leishmania donovani, and principal components analysis was used to cluster compounds on potential mode of action, offering a medium throughput screening approach in drug selection/prioritization. The comprehensive and sensitive nature of the data has also made detailed effects of each compound obtainable, providing a resource to assist in further mechanistic studies and prioritization of these compounds for the development of new antileishmanial drugs.


Asunto(s)
Antiprotozoarios/uso terapéutico , Descubrimiento de Drogas , Leishmaniasis/tratamiento farmacológico , Antiprotozoarios/química , Análisis por Conglomerados , Evaluación Preclínica de Medicamentos/métodos , Electroforesis Capilar , Ensayos Analíticos de Alto Rendimiento , Leishmania donovani/efectos de los fármacos , Leishmania donovani/metabolismo , Espectrometría de Masas , Metabolómica , Análisis de Componente Principal , Proteínas Protozoarias/metabolismo
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