Label-free screening assays: a strategy for finding better drug candidates

被引:9
|
作者
Lunn, Charles A. [1 ]
机构
[1] New Lead Discovery Merck Res Labs, Kenilworth, NJ 07033 USA
关键词
SCINTILLATION PROXIMITY ASSAY; HETEROTRIMERIC G-PROTEINS; SMALL-MOLECULE ACTIVATORS; CANNABINOID RECEPTOR; MASS-SPECTROMETRY; FUNCTIONAL SELECTIVITY; ALLOSTERIC MODULATORS; STEM-CELLS; BONE MASS; CB2;
D O I
10.4155/FMC.10.246
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The last 10 years have seen advances in automation and high-throughput biochemistry in the drug-discovery arena However, these advances have not led to improvements in drug-discovery success Drug programs must find new ways to identify superior compounds Advances in label-free assay technologies may provide advantages needed for improved drug discovery In this article, we will discuss high-throughput MS, a technology that allows screening with native substrates and with targets inaccessible to standard assay formats We will then discuss cell-based label-free biosensors, focusing on the increased information content available when using these platforms We will conclude with speculation on the future and ways to obtain relevant biological information early in development to ensure the best compounds are promoted to medicinal chemistry campaigns
引用
收藏
页码:1703 / 1716
页数:14
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