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Epigenetic Screening

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Profile with the Industry's Largest Epigenetics Portfolio

Epigenetics, an increasingly popular field of drug discovery, is the study of heritable changes in gene expression that occur without changes in the DNA sequence. The epigenome is considered to be in constant flux and is responsive to environmental and pharmaceutically active molecules. Epigenetics-related enzymes and proteins catalyze the addition or removal of an array of covalent modifications on histone and non-histone proteins. For these reasons, epigenetics is becoming an increasingly important realm for drug therapies. Indeed, several drugs directed towards epigenetic modifying enzymes are already on the market with more in the clinic to treat cancer.

In 2012, ahead of all other CROs, Eurofins recognized the industry's upcoming need for a comprehensive epigenetics program containing all major families. To meet this growing need, we began to develop a range of target based assays using biologically relevant substrates (nucleosomes, histones, and peptides) to create the most meaningful assays. The majority of our proteins/substrates are produced in-house to ensure the highest quality of proteins resulting in high batch to batch reproducibility.

Eurofins' epigenetic toolbox is based on several technology platforms and allows for your choice of technology and/or substrates, providing added flexibility to meet all of your drug discovery needs.

Advantages of Eurofins' Epigenetics Program:

  • Largest target and assay list in the industry, with over 160 epigenetic assays to choose from:
    • >50 Writers,  including: SMMT, Kinases, DNMT, HMT and HAT
    • >40 Erasers, including: Demethylases, HDAC / sirtuin and DUB
    • >45 Readers, including: Bromodomain and Methyl readers
    • >17 Off-target and cell-based assays, including acetylation and methylation studies
  • Compatible with screening in medium- or high-throughput
  • All assays set up according to NIH guidelines
    • Employing biologically-relevant co-factors and substrates
    • Assay optimization includes apparent Km identification for assay constituents and assay linearization
  • Assays can be modified to meet client needs
  • Several technology platforms cover the epigenetic portfolio:
    • Gold standard filter-based radioactivity
    • RapidFire Mass Spectrometry
    • AlphaScreen
    • TR-FRET
  • Customer tailored assays to supplement our off-the-shelf assay portfolio
    • A specific protein can be cloned, expressed, purified and have a corresponding enzymatic or binding assay developed using a selected technology platform



Figures 1. PRMT7 histone methyltransferase - an example of our assay development process

Kinetic assays (top panel) are performed to determine the assay's linear range. The arrow indicates the time at which the reaction is stopped. The assay resulting from our development process can easily detect reference compounds (bottom panel). Developed assays, such as this one, are performed using Km values for both substrates and co-factors.