Reliable high-throughput functional screening with 3-FABS

被引:51
作者
Dalvit, C
Ardini, E
Fogliatto, GP
Mongelli, N
Veronesi, M
机构
[1] Nerviano Med Sci, Dept Chem, I-20014 Nerviano, MI, Italy
[2] Nerviano Med Sci, Dept Biol, I-20014 Nerviano, MI, Italy
关键词
D O I
10.1016/S1359-6446(04)03161-7
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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 (IC50) with accuracy. The substrate is tagged with a CF3 moiety and F-19 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.
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页码:595 / 602
页数:8
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