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Fluorine NMR functional screening: from purified enzymes to human intact living cells

Dalvit, Claudio and Veronesi, Marina and Vulpetti, Anna (2020) Fluorine NMR functional screening: from purified enzymes to human intact living cells. Journal of Biomolecular NMR. ISSN 15735001

Abstract

The substrate- or cofactor-based fluorine NMR screening, also known as n-FABS (n fluorine atoms for biochemical screening), represents a powerful method for performing a direct functional assay in the search of inhibitors or enhancers of an enzymatic reaction. Although it suffers from the intrinsic low sensitivity compared to other biophysical techniques usually applied in functional assays, it has some distinctive features that makes it appealing for tackling complex chemical and biological systems. Its strengths are represented by the easy set-up, robustness, flexibility, lack of signal interference and rich information content resulting in the identification of bona fide inhibitors and reliable determination of their inhibitory strength. The versatility of the n-FABS allows its application to either purified enzymes, cell lysates or intact living cells. The principles, along with theoretical, technical and practical aspects, of the methodology are discussed. Furthermore, several applications of the technique to pharmaceutical projects are presented.

Item Type: Article
Keywords: 19F NMR spectroscopy Fluorinated substrates Fragment based drug discovery (FBDD) Functional assay IC50 determination Living cells n fluorine atoms for biochemical screening (n-FABS)
Date Deposited: 26 May 2020 00:45
Last Modified: 26 May 2020 00:45
URI: https://oak.novartis.com/id/eprint/41750

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