Screening for Inhibitors of the Ubiquitination Regulator and Anticancer Target CSN5 using a HTS Fluorescence Polarization Method
20 Jul 2017The application note describes the design and performance of a biochemical protease assay to probe the activity of the anticancer target, CSN5. The aim was to create a high-throughput screening assay to identify chemical starting points for drug discovery. The PHERAstar® FSX was used to a carry out a fluorescence polarization and TR-FRET assay. The high sensitivity of the PHERAstar® FSX reader together with the simultaneous detection of both emission channels enabled for fast FP measurements, allowing the assay to be run in a continuous manner, resulting in a highly efficient workflow.
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High-Throughput ScreeningHigh-throughput screening (HTS) is an automated drug discovery technique for identification of active compounds against a compound library. Use HTS readers and integrated assay preparation / analysis workstations to screen your compounds. Identify active compounds against various HTS libraries, including membranes, proteins and peptides and HTS cell lines. Find the best high-throughput screening products in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.Microplate Readers / DetectorsMicroplate readers are used to automate the detection and analysis of labeled or label-free components in microplates during assays or live-cell monitoring. Microplate readers are generally distinguished by their mode of detection. Types include absorbance, luminescence, fluorescence intensity, fluorescence polarization, TRF / FRET and multimode microplate readers. Microplate readers deliver a high throughput of samples by reading multiple wells simultaneously, with the 96-well format the most commonly used. As a result, microplate readers are often used in the drug discovery, bioassays, research and pharmaceutical industries for screening applications. Microplate loading can also be automated, with robotic microplate stackers to increase throughput. Find the best microplate readers in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.Assay AssemblyAssay Assembly is technique used in drug discovery to develop assays to test the cytotoxicity, genotoxicity, or other activities of a compound on a cell. Assay assembly requires chip assembly, a delivery system and a detection and analysis method. Beneficial features of assay kits or automated systems include high-throughput, high speed and sensitivity and low signal to noise ratio.Compound LibrariesCompound libraries, or chemical libraries, are used in drug discovery for the identification of potential therapeutics compounds. Used in conjunction with high-throughput screening, the libraries of stored compounds are often generated for specific purposes as a drug target or disease model. Cheminformatics are commonly used when designing a compound library and software can be used to analyze the screening process. Fluorescence Based AssayFluorescence based assays are widely used in life science research and high-throughput screening to measure a broad range of cellular activities.High ThroughputHigh throughput experiments allow the simultaneous processing of several samples. This parallelization reduces the cost per experiment and increases reproducibility and output volume of data.Assay DevelopmentThe process of proving an assay to be sensitive with respect to the target is known as assay development. The assay should be able to characterize novel compounds and measure the potency of these compounds against a validated biological target.TR-FRETFRETCompound ScreeningCompound screening is a method used to discover specific compounds that could be promising candidates for pharmaceutical use. This potential is identified when compounds interact with the target protein during screening and could therefore be carried forward in the drug development process.