Probing the interaction of a quercetin bioconjugate with Bcl-2 in living human cancer cells with in-cell NMR spectroscopy

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Title
Probing the interaction of a quercetin bioconjugate with Bcl-2 in living human cancer cells with in-cell NMR spectroscopy
Author(s)
A Primikyri; N Sayyad; G Quilici; E Vrettos; Kyungeun Lim; Seung-Wook Chi; G Musco; I P Gerothanassis; A G Tzakos
Bibliographic Citation
FEBS Letters, vol. 592, no. 20, pp. 3367-3379
Publication Year
2018
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.
Keyword
STDBcl-2Tr-NOESYin-cell NMRquercetin-alanine bioconjugate
ISSN
0014-5793
Publisher
Wiley
DOI
http://dx.doi.org/10.1002/1873-3468.13250
Type
Article
Appears in Collections:
Division of Biomedical Research > 1. Journal Articles
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