A recent article in Scientific Advances describes the utility of dTect™, EpiCypher’s latest technology to identify novel enzyme targets. These libraries are comprised of a diverse set of approximately 47 million degenerate peptide substrates to characterize lysine methyltransferase (KMT) activity and selectivity.
Research Triangle Park, NC – 28 November 2018 – A recent article in Scientific Advances describes the utility of dTect™, EpiCypher’s latest technology to identify novel enzyme targets. These libraries are comprised of a diverse set of approximately 47 million degenerate peptide substrates to characterize lysine methyltransferase (KMT) activity and selectivity. This innovative, high-throughput platform revealed many novel KMT target motifs, which were enriched for residues often masked by standard mass-spectrometry (MS) techniques, demonstrating the advantages of this technology for basic research and drug discovery applications.
The pace of lysine methylation research has accelerated, with over 6,000 unique methyl sites described on 3,000 distinct proteins. Targeting the enzymes that catalyze these marks for therapeutic intervention requires thorough knowledge of KMT substrate specificity, which is typically defined by MS analyses. Despite the power of this technique, it is still a time-consuming, expensive and inaccessible technique for many laboratories and hospitals. As illustrated in the article, MS also misses a large subset of important motifs, largely due to the chemical properties of certain amino acids. In fact, the weaknesses of the mass spec system appear to directly impede detection of the most robust KMT motifs detected by dTect™.
“These results highlight the need for additional resources in the field of epigenetics drug development, and complement EpiCypher’s growing role in the creation of highly innovative, unbiased tools for epigenetics research,” said Dr. Michael-Christopher Keogh, Chief Scientific Officer at EpiCypher. “We expect dTect™ to become a standard high-throughput discovery approach, as it can be adapted for many types of enzymes, and across multiple areas of biomedical research.”
dTect™ is a fully customizable service, enabling scientists to screen any number of peptide substrates for their lysine- or arginine-targeting enzyme of interest. As shown in the Scientific Advances report, this approach can be used to identify novel KMT targets, design highly precise inhibitors, and prioritize cancer proteomic mutations, making the platform particularly useful for pharmaceutical and clinical research.
About EpiCypher - A pioneer in the field of epigenetics and chromatin biology, EpiCypher® is a biotechnology company developing transformative technologies to researchers and drug developers worldwide. EpiCypher manufactures and sells a series of products and assay platforms that use recombinant “designer” modified nucleosomes (dNucs), including the SNAP-ChIP® product family for quantitative ChIP applications and the EpiDyne® product family for nucleosome remodeling assays, as well as recombinant histone binding proteins and enzymes, peptides and antibodies, and offers a broad range of custom substrate manufacturing and assay development services.
Media contact:
Ana Aza, PhD
Marketing Manager
ana@epicypher.com
