期刊
FEBS LETTERS
卷 592, 期 20, 页码 3367-3379出版社
WILEY
DOI: 10.1002/1873-3468.13250
关键词
Bcl-2; in-cell NMR; quercetin-alanine bioconjugate; STD; Tr-NOESY
资金
- State Scholarships Foundation of Greece - Act 'Supporting Postdoctoral Researchers' from the resources of the NF 'Human Resources Development, Education and Lifelong Learning'
- European Social Fund -ESF
- Greek State
- NRF grant - Korea Government (MSIT) [NRF-2017R1E1A1A01074403]
- European Union (European Social Fund ESF)
- Greek national funds through the Operational Program Education and Lifelong Learning of the National Strategic Reference Framework (NSRF) - Research Funding Program: ARISTEIA II [5199]
- National Research Foundation of Korea [2017R1E1A1A01074403] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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.
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