Automating a Direct, Cell-Based, Target-Compound Interaction Assay for G9a Histone Methyltransferase and Bromodomain Proteins

11 Feb 2013

This application note describes a novel, cell-based assay platform that uses Enzyme Fragment Complementation (EFC) Technology to detect the specific binding and direct protein engagement of potential small molecule inhibitors to G9a methyltransferase and multiple bromodomain proteins. The combination of assay chemistry and liquid handling and detection microplate instrumentation create a simple, robust and definitive cell-based solution for inhibitory compound identification of these important epigenetic targets.

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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.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.  Cell-Based AssaysCell-based assays are used to monitor the presence, quantity and activities of a desired cellular analyte including drug molecules or biomarkers. This can reveal information on cell health (apoptosis, cytotoxicity, viability and proliferation assays), cell metabolism, cell migration and cell signaling mechanisms. Find the best cell-based assay products, kits and equipment with our peer reviewed product directory: compare products, check customer reviews and receiving pricing direct from manufacturers.High-Content ScreeningHigh-content screening (HCS), also known as high-content analysis (HCA), is a high-throughput technique used in drug discovery to identify substances that alter the phenotype of cells. HCS uses fluorescent microscopic imaging and automated image analysis to investigate cellular events such as apoptosis, cell viability, GPCR activation, oxide production, neurite outgrowth, and cell signaling. Find the best fluorescent labeling reagents, cellular assays, and high-content imaging systems in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.Epigenetic AnalysisEpigenetic analysis products are used to study heritable phenotype changes that do not alter the DNA sequence, such as DNA modifications affecting gene activity. Determine whether genes have been methylated with DNA methylation quantification kits or methylation microarrays. Assess epigenetic regulation with histone modification kits or ChIP-on-chip microarrays. Kits are also available for bisulfite conversion and amplification of your samples, as well as epigenomic library preparation kits for next-generation sequencing (NGS). Find the best epigenetic products in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.MethylationHistone ModificationInhibitorsCompound 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.
Automating a Direct, Cell-Based, Target-Compound Interaction Assay for G9a Histone Methyltransferase and Bromodomain Proteins