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      Fluorescence polarization assays in high-throughput screening and drug discovery: a review

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          Abstract

          <p class="first" id="P1">The sensitivity of Fluorescence Polarization (FP) and Fluorescence Anisotropy (FA) to molecular weight changes has enabled the interrogation of diverse biological mechanisms, ranging from molecular interactions to enzymatic activity. Assays based on FP/FA technology have been widely utilized in high-throughput screening (HTS) and drug discovery due to the homogenous format, robust performance and relative insensitivity to some types of interferences, such as inner filter effects. Advancements in assay design, fluorescent probes, and technology have enabled the application of FP assays to increasingly complex biological processes. Herein we discuss different types of FP/FA assays developed for HTS, with examples to emphasize the diversity of applicable targets. Furthermore, trends in target and fluorophore selection, as well as assay type and format, are examined using annotated HTS assays within the PubChem database. Finally, practical considerations for the successful development and implementation of FP/FA assays for HTS are provided based on experience at our center and examples from the literature, including strategies for flagging interference compounds among a list of hits. </p>

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          Most cited references92

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          A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays

          J-H Zhang (1999)
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            Bright ideas for chemical biology.

            Small-molecule fluorescent probes embody an essential facet of chemical biology. Although numerous compounds are known, the ensemble of fluorescent probes is based on a modest collection of modular "core" dyes. The elaboration of these dyes with diverse chemical moieties is enabling the precise interrogation of biochemical and biological systems. The importance of fluorescence-based technologies in chemical biology elicits a necessity to understand the major classes of small-molecule fluorophores. Here, we examine the chemical and photophysical properties of oft-used fluorophores and highlight classic and contemporary examples in which utility has been built upon these scaffolds.
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              High-throughput screening assays for the identification of chemical probes.

              High-throughput screening (HTS) assays enable the testing of large numbers of chemical substances for activity in diverse areas of biology. The biological responses measured in HTS assays span isolated biochemical systems containing purified receptors or enzymes to signal transduction pathways and complex networks functioning in cellular environments. This Review addresses factors that need to be considered when implementing assays for HTS and is aimed particularly at investigators new to this field. We discuss assay design strategies, the major detection technologies and examples of HTS assays for common target classes, cellular pathways and simple cellular phenotypes. We conclude with special considerations for configuring sensitive, robust, informative and economically feasible HTS assays.
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                Author and article information

                Journal
                Methods and Applications in Fluorescence
                Methods Appl. Fluoresc.
                IOP Publishing
                2050-6120
                June 01 2016
                April 28 2016
                : 4
                : 2
                : 022001
                Article
                10.1088/2050-6120/4/2/022001
                5563979
                28809163
                cae8a8e5-2ac1-4beb-964f-313eb99863b1
                © 2016

                http://iopscience.iop.org/info/page/text-and-data-mining

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