Fragment-Based Screening of a Natural Product Library against 62 Potential Malaria Drug Targets Employing Native Mass Spectrometry.
ACS Infect Dis
; 4(4): 431-444, 2018 04 13.
Article
em En
| MEDLINE
| ID: mdl-29436819
Natural products are well known for their biological relevance, high degree of three-dimensionality, and access to areas of largely unexplored chemical space. To shape our understanding of the interaction between natural products and protein targets in the postgenomic era, we have used native mass spectrometry to investigate 62 potential protein targets for malaria using a natural-product-based fragment library. We reveal here 96 low-molecular-weight natural products identified as binding partners of 32 of the putative malarial targets. Seventy-nine (79) fragments have direct growth inhibition on Plasmodium falciparum at concentrations that are promising for the development of fragment hits against these protein targets. This adds a fragment library to the published HTS active libraries in the public domain.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Plasmodium falciparum
/
Espectrometria de Massas
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Produtos Biológicos
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Avaliação Pré-Clínica de Medicamentos
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Antimaláricos
Tipo de estudo:
Diagnostic_studies
/
Screening_studies
Idioma:
En
Revista:
ACS Infect Dis
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Austrália