Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 60, Issue 36, Pages 19637-19642Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202104947
Keywords
analytical methods; drug discovery; drug screening; mass spectrometry; protein analysis
Categories
Funding
- Israel Science Foundation (ISF) [300/17]
- Sagol Institute for Longevity Research grant
- Moross Proof-of-Concept grant
- Ephraim Katzir Memorial Professorial Chair
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Researchers have developed a method based on native mass spectrometry for analyzing drug uptake and target engagement in cellular contexts. This approach utilizes direct MS for label-free studies of protein-drug binding in human cells.
Understanding protein-ligand interactions in a cellular context is an important goal in molecular biology and biochemistry, and particularly for drug development. Investigators must demonstrate that drugs penetrate cells and specifically bind their targets. Towards that end, we present a native mass spectrometry (MS)-based method for analyzing drug uptake and target engagement in eukaryotic cells. This method is based on our previously introduced direct-MS method for rapid analysis of proteins directly from crude samples. Here, direct-MS enables label-free studies of protein-drug binding in human cells and is used to determine binding affinities of lead compounds in crude samples. We anticipate that this method will enable the application of native MS to a range of problems where cellular context is important, including protein-protein interactions, drug uptake and binding, and characterization of therapeutic proteins.
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