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Fluorine nuclear magnetic resonance-based assay in living mammalian cells.
Journal article

Fluorine nuclear magnetic resonance-based assay in living mammalian cells.

  • Veronesi M Department of Drug Discovery and Development, Fondazione Istituto Italiano di Tecnologia, 16163 Genoa, Italy. Electronic address: marina.veronesi@iit.it.
  • Giacomina F Department of Drug Discovery and Development, Fondazione Istituto Italiano di Tecnologia, 16163 Genoa, Italy.
  • Romeo E Department of Drug Discovery and Development, Fondazione Istituto Italiano di Tecnologia, 16163 Genoa, Italy.
  • Castellani B Department of Drug Discovery and Development, Fondazione Istituto Italiano di Tecnologia, 16163 Genoa, Italy.
  • Ottonello G Department of Drug Discovery and Development, Fondazione Istituto Italiano di Tecnologia, 16163 Genoa, Italy.
  • Lambruschini C Department of Drug Discovery and Development, Fondazione Istituto Italiano di Tecnologia, 16163 Genoa, Italy.
  • Garau G Department of Drug Discovery and Development, Fondazione Istituto Italiano di Tecnologia, 16163 Genoa, Italy.
  • Scarpelli R Department of Drug Discovery and Development, Fondazione Istituto Italiano di Tecnologia, 16163 Genoa, Italy.
  • Bandiera T Department of Drug Discovery and Development, Fondazione Istituto Italiano di Tecnologia, 16163 Genoa, Italy.
  • Piomelli D Department of Drug Discovery and Development, Fondazione Istituto Italiano di Tecnologia, 16163 Genoa, Italy; Department of Anatomy and Neurobiology, School of Medicine, University of California, Irvine, Irvine, CA 92697, USA.
  • Dalvit C Institut de Chimie, Faculté des Sciences, Université de Neuchâtel, 2000 Neuchâtel, Switzerland.
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  • 2015-12-22
Published in:
  • Analytical biochemistry. - 2016
(19)F NMR screening
IC(50)
Mammalian cells
Metabolic fingerprint
hFAAH
n-FABS
Amidohydrolases
Benzamides
Carbamates
Fluorine
HEK293 Cells
Humans
Inhibitory Concentration 50
Nuclear Magnetic Resonance, Biomolecular
English 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.
Language
  • English
Open access status
closed
Identifiers
Persistent URL
https://sonar.ch/global/documents/278124
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