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Enabling Epigenetics Studies from HTS to SAR: a Novel HTRF® Platform to Identify and Characterize Reader Domain Inhibitors

Cisbio Bioassays
23 Sept 2014

This poster describes a novel assay platform based on HTRF technology which enables the discovery and the characterization of novel reader domain inhibitors. More than 20 different assays have been built up to monitor the interaction of Bromodomain, Tudor domains, MBT domains and Chromodomains with histone peptides.

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EPIgeneous™ Binding Domain Assays

Cisbio Bioassays

EPIgeneous™ Binding Domain Assay Kits for studying epigenetic readers. This biochemical assay platform enables a no-wash, sensitive, reliable detection of protein/protein interaction between epigenetic binding domains and histone sequences modified by epigenetic enzymes. Three assay kits (A, B and C) have already been validated and fully optimized on a selection of 28 key binding domains. For non-validated reader domains, a fourth kit (Discovery) enables you to profile which of the A, B or C kits is the best assay solution. All kits are based on a GST-tagged Binding Domain /biotin-coupled Histone peptide format, and can be run using the same mix-and-read single plate protocol. EPIgeneous™ Binding domain assay kits are ideal assay tools for both primary and secondary screening as well as for further inhibitor studies.Features: Fully optimized on 28 key reader proteins High sensitivity and robustness for inhibitor screening Good DMSO tolerance Low consumption of protein and peptide Applications: Bromodomain, Chromodomain, Tudordomain & MBT domain assays High Throughput Screening Inhibitor profiling

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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.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.Protein PurificationProtein purification is a vital step in drug discovery, therapeutics, biotech and life science research. The purification process typically involves subcellular or membrane protein extraction with cell lysis kits, separation of proteins from cell debris by filtration or spin columns, and the isolation of proteins of interest from other proteins and impurities with affinity purification (including fusion protein tags and antibody binding proteins A, G and L), immunoprecipitation or chromatographic methods, such as ion exchange, size exclusion and immobilized metal affinity chromatography. All purification methods come in multiple formats for your laboratory needs, including agarose or magnetic beads, resins, columns and filter plates. Find the best protein purification equipment 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.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.ScreeningUsing robotics, data processing and control software, liquid handling devices and sensitive detectors, screening allows a researcher to quickly conduct millions of chemical, genetic or pharmacological tests.

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