Probing the interaction of a quercetin bioconjugate with Bcl‐2 in living human cancer cells with in‐cell NMR spectroscopy. Issue 20 (29th September 2018)

• Record Type: Journal Article
• Authors: Primikyri, Alexandra; Sayyad, Nisar; Quilici, Giacomo; Vrettos, Eirinaios I.; Lim, Kyungeun; Chi, Seung‐Wook; Musco, Giovanna; Gerothanassis, Ioannis P.; Tzakos, Andreas G.
• Is Part Of: FEBS letters. Volume 592:Issue 20(2018)
• Page Start: 3367
• Page End: 3379
• Publication Date: 2018-09-29
• Subjects: Bcl‐2 -- in‐cell NMR -- quercetin‐alanine bioconjugate -- STD -- Tr‐NOESY; Biochemistry -- Periodicals; Biophysics -- Periodicals; Molecular biology -- Periodicals; Biochimie -- Périodiques; Biochemistry; Biophysics; Molecular biology; Periodicals; 572.05
• DOI: 10.1002/1873-3468.13250
• Languages: English
• ISSNs: 0014-5793

Abstract

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. Abstract :