小分子筛选中的荧光偏振测定法。
Fluorescence polarization assays in small molecule screening.
机构信息
National Human Genome Research Institute, National Institutes of Health, NIH Chemical Genomics Center, Bethesda, MD 20892-3370, USA.
出版信息
Expert Opin Drug Discov. 2011 Jan;6(1):17-32. doi: 10.1517/17460441.2011.537322.
IMPORTANCE OF THE FIELD
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 have been symbolized by the facile adoption of FP in high-throughput screening and small molecule drug discovery of an increasing range of target classes.
AREAS COVERED IN THIS REVIEW
The article provides a brief overview of the theoretical foundation of FP, followed by updates on recent advancements in its application for various drug target classes, including GPCRs, enzymes and protein-protein interactions. The strengths and weaknesses of this method, practical considerations in assay design, novel applications and future directions are also discussed.
WHAT THE READER WILL GAIN
The reader is informed of the most recent advancements and future directions of FP application to small molecule screening.
TAKE HOME MESSAGE
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.
重要性的领域
荧光偏振（FP）是一种均相的方法，允许快速和定量分析的各种分子相互作用和酶活性。这项技术已被广泛应用于临床和生物医学领域，包括某些疾病的诊断和监测治疗药物在体液中的水平。该领域的最新进展的特点是轻松采用 FP 在高通量筛选和小分子药物发现的不断增加的目标类别。
涵盖的领域在这篇综述中
文章提供了一个简要概述的理论基础的 FP，接着更新其应用的最新进展的各种药物靶类，包括 GPCRs、酶和蛋白质-蛋白质相互作用。该方法的优缺点，在设计中的实际考虑assay，新的应用和未来的方向也进行了讨论。
读者将获得什么
读者将获得最新的进展和未来的方向的 FP 应用于小分子筛选。
带回家的消息
除了其在高通量筛选中的持续应用，FP 已经扩展到新的疾病和靶区，并以标记的小分子配体用于受体结合研究的使用增加为标志。
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