Burke T J, Loniello K R, Beebe J A, Ervin K M
PanVera LLC, 501 Charmany Drive, Madison, WI 53719, USA.
Comb Chem High Throughput Screen. 2003 May;6(3):183-94. doi: 10.2174/138620703106298365.
Fluorescence polarization technology has been used in basic research and commercial diagnostic assays for many decades, but has begun to be widely used in drug discovery only in the past six years. Originally, FP assays for drug discovery were developed for single-tube analytical instruments, but the technology was rapidly converted to high-throughput screening assays when commercial plate readers with equivalent sensitivity became available. This review will discuss fluorescence polarization assays in current use in drug discovery research as well as those in development that will likely be used in the near future. These assays include targets such as kinases, phosphatases, proteases, G-protein coupled receptors, and nuclear receptors.
几十年来,荧光偏振技术一直应用于基础研究和商业诊断检测,但仅在过去六年才开始广泛应用于药物研发。最初,用于药物研发的荧光偏振检测是为单管分析仪器开发的,但当具有同等灵敏度的商用酶标仪出现后,该技术迅速转变为高通量筛选检测。本综述将讨论目前在药物研发研究中使用的荧光偏振检测方法,以及那些可能在不久的将来会被使用的正在开发中的检测方法。这些检测方法包括针对激酶、磷酸酶、蛋白酶、G蛋白偶联受体和核受体等靶点。