Fluorine nuclear magnetic resonance-based assay in living mammalian cells
| Autor: | Daniele Piomelli, Claudio Dalvit, Tiziano Bandiera, Beatrice Castellani, Elisa Romeo, Chiara Lambruschini, Rita Scarpelli, Giuliana Ottonello, Gianpiero Garau, Francesca Giacomina, Marina Veronesi |
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| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Nuclear Magnetic Resonance Cell Metabolic fingerprint Biophysics Fluorine-19 NMR IC50 010402 general chemistry 01 natural sciences Biochemistry Amidohydrolases 03 medical and health sciences Inhibitory Concentration 50 Nuclear magnetic resonance Fatty acid amide hydrolase medicine Humans Receptor Nuclear Magnetic Resonance Biomolecular Molecular Biology Chemistry Drug discovery HEK 293 cells Mammalian cells hFAAH Fluorine Cell Biology 19F NMR screening n-FABS Benzamides Carbamates HEK293 Cells 0104 chemical sciences 030104 developmental biology medicine.anatomical_structure Membrane protein Biomolecular |
| Zdroj: | Veronesi, M; Giacomina, F; Romeo, E; Castellani, B; Ottonello, G; Lambruschini, C; et al.(2016). Fluorine nuclear magnetic resonance-based assay in living mammalian cells. Analytical Biochemistry, 495, 52-59. doi: 10.1016/j.ab.2015.11.015. UC Irvine: Retrieved from: http://www.escholarship.org/uc/item/31j1k53g |
| Popis: | © 2015 Elsevier Inc. All rights reserved. Nuclear magnetic resonance (NMR)-based screening has been recognized as a powerful approach for the identification and characterization of molecules interacting with pharmaceutical targets. Indeed, several NMR methods have been developed and successfully applied to many drug discovery projects. Whereas most of these approaches have targeted isolated biomolecular receptors, very few cases are reported with the screening performed in intact cells and cell extracts. Here we report the first successful application of the fluorine NMR-based assay n-FABS (n-fluorine atoms for biochemical screening) in living mammalian cells expressing the membrane protein fatty acid amide hydrolase (FAAH). This method allows the identification of both weak and potent inhibitors and the measurement of their potency in a physiological environment. |
| Databáze: | OpenAIRE |
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