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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

Authors 

A PrimikyriN SayyadG QuiliciE VrettosKyungeun LimSeung-Wook ChiG MuscoI P GerothanassisA G Tzakos

Publisher 

Elsevier

Issue Date 

2018

Citation 

FEBS Letters

Keywords 

STDBcl-2Tr-NOESYin-cell NMRquercetin-alanine bioconjugate

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.

ISSN 

0014-5793

Link 

http://dx.doi.org/10.1002/1873-3468.13250

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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