Reliable high-throughput functional screening with 3-FABS.
An NMR method called 3-FABS has extended the capabilities of NMR, enabling rapid, efficient and reliable high-throughput functional screening for the identification of inhibitors and for measuring their 50% mean inhibition concentration (IC(50)) with accuracy. The substrate is tagged with a CF(3) moiety and (19)F NMR spectroscopy is used for the detection of the substrate and product components. We provide comprehensive insight into 3-FABS, a discussion of its strength and weakness when compared with other HTS techniques and a presentation of some of its applications to the screening of different enzymes and to multiple screening.
Dalvit
Claudio
C
Chemistry Department, Nerviano Medical Science, Viale Pasteur 10, 20014 Nerviano (MI), Italy. claudio.dalvit@nervianoms.com
Ardini
Elena
E
Fogliatto
Gian Paolo
GP
Mongelli
Nicola
N
Veronesi
Marina
M
D004353:Drug Evaluation, Preclinical / Q000379:methods*; D005462:Fluorine Radioisotopes; D009682:Magnetic Resonance Spectroscopy / Q000379:methods*; D013379:Substrate Specificity; D013678:Technology, Pharmaceutical / Q000379:methods*
D005462:Fluorine Radioisotopes