Probing the interaction of a quercetin bioconjugate with Bcl-2 in living human cancer cells with in-cell NMR spectroscopy.
FEBS Lett
; 592(20): 3367-3379, 2018 10.
Article
em En
| MEDLINE
| ID: mdl-30207377
ABSTRACT
In-cell NMR spectroscopy has emerged as a powerful technique for monitoring biomolecular interactions at an atomic level inside intact cells. However, current methodologies are inadequate at charting intracellular interactions of nonlabeled proteins and require their prior isotopic labeling. Herein, we describe for the first time the monitoring of the quercetin-alanine bioconjugate interaction with the nonlabeled antiapoptotic protein Bcl-2 inside living human cancer cells. STD and Tr-NOESY in-cell NMR methodologies were successfully applied in the investigation of the binding, which was further validated in vitro. In-cell NMR proved a very promising strategy for the real-time probing of the interaction profile of potential drugs with their therapeutic targets in native cellular environments and could, thus, open a new avenue in drug discovery.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Quercetina
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Espectroscopia de Ressonância Magnética
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Proteínas Proto-Oncogênicas c-bcl-2
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Alanina
Limite:
Humans
Idioma:
En
Revista:
FEBS Lett
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Grécia