Fluorescence polarization assays in small molecule screening.
Fluorescence polarization assays in small molecule screening.
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DOI：
10.1517/17460441.2011.537322
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发表时间：
2011-01
影响因子：
6.3
通讯作者：
Simeonov A
中科院分区：
文献类型：
--
作者：
Lea WA;Simeonov A
荧光极化（FP）是一种均匀的方法，可以快速定量分析各种分子相互作用和酶活性。这项技术已广泛用于临床和生物医学环境，包括诊断某些疾病和监测体液中的治疗药物水平。该领域最近的发展标志着FP在高通量筛选（HTS）和越来越多靶点类别的小分子药物发现中的应用。本文简要介绍了FP的理论基础，随后介绍了其在各种药物靶点类别中的应用进展，包括g蛋白偶联受体（gpcr）、酶和蛋白-蛋白相互作用（PPIs）。本文还讨论了该方法的优点和缺点、分析设计中的实际考虑、新的应用和未来的发展方向。读者将了解FP在小分子筛选中的最新进展和未来发展方向。除了继续用于高通量筛选外，FP已扩展到新的疾病和靶标领域，并且在受体结合研究中越来越多地使用标记的小分子配体。
Fluorescence polarization (FP) is a homogeneous method that allows rapid and quantitative analysis of diverse molecular interactions and enzyme activities. This technique has been widely utilized in clinical and biomedical settings, including the diagnosis of certain diseases and monitoring therapeutic drug levels in body fluids. Recent developments in the field has been symbolized by the facile adoption of FP in high-throughput screening (HTS) and small molecule drug discovery of an increasing range of target classes. The article provides a brief overview on the theoretical foundation of FP, followed by updates on recent advancements in its application for various drug target classes, including G-protein coupled receptors (GPCRs), enzymes and protein-protein interactions (PPIs). The strengths and weaknesses of this method, practical considerations in assay design, novel applications, and future directions are also discussed. The reader will be informed of the most recent advancements and future directions of FP application to small molecule screening. In addition to its continued utilization in high-throughput screening, FP has expanded into new disease and target areas and has been marked by increased use of labeled small molecule ligands for receptor binding studies.
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影响因子：
14.9
作者：
Cer RZ;Mudunuri U;Stephens R;Lebeda FJ
通讯作者：
Lebeda FJ
影响因子：
4.3
作者：
Cao, ZH;Tan, WH
通讯作者：
Tan, WH
基于锥虫RNA三磷酸酶TBCET1的高密度荧光极化测定的开发和验证。
DOI：
10.2174/138620709787581729
发表时间：
2009-03
影响因子：
1.8
作者：
Antczak C;Shum D;Radu C;Seshan VE;Djaballah H
通讯作者：
Djaballah H
影响因子：
1.8
作者：
Beasley, JR;Dunn, DA;Auld, DS
通讯作者：
Auld, DS
影响因子：
2.9
作者：
Collazo, E;Couture, JF;Trievel, RC
通讯作者：
Trievel, RC