BellBrook Labs, an innovative developer of drug discovery tools, is launching a new Transzyme Methyltransferase Assay kit for EZH2, an oncogenic histone methyltransferase that is being targeted for non-small cell lung cancer and other types of cancer. The new Transzyme EZH2 Assay combines the company’s Transcreener HTS assay technology with Reaction Biology’s purified EZH2 enzyme to provide a complete methyltransferase assay solution for inhibitor high throughput screening (HTS) and profiling.
Madison, WI (PRWEB) August 28, 2013 -- BellBrook Labs is continuing their successful collaboration with Reaction Biology to accelerate epigenetics drug discovery with the launch of a new Transzyme Methyltransferase Assay kit for histone methyltransferase EZH2. The Transzyme EZH2 kit combines all of the required EZH2 enzyme reaction components and BellBrook’sTranscreener EPIGEN Methyltransferase Assay detection reagents into a well-defined kit that is pre-calibrated to produce HTS-quality data. With the addition of EZH2, the expanding line of Transzyme Methyltransferase Assays now numbers fourteen, including DOT1L, G9a, MLL4, PRMT1, PRMT3 SET7/9, SET8, SUVH391 and DNMT1. By eliminating the need for sourcing and testing of reagents from different vendors and trouble-shooting to optimize assay performance, the new Transzyme kits should accelerate the pursuit of promising epigenetic therapeutic strategies for cancer and other diseases.
Methyltransferases are key players in epigenetic control of gene expression and have become the targets of intensive public and private drug discovery efforts. Unfortunately, the first step in developing epigenetic drugs – identification of specific inhibitors for target enzymes – has been plagued by problems in getting methyltransferase enzymes to function correctly in the HTS assays used to detect their activity. To eliminate this hurdle, BellBrook Labs and Reaction Biology partnered last year to develop the Transzyme Methyltransferase Assay kits as complete solutions for inhibitor screening and profiling with purified methyltransferases enzymes.
EZH2 is a complex of five different proteins that act in concert to catalyze mono-, di- and tri-methylation of Histone 3 at Lys 27. The tri-methyl H3K27 mark causes transcriptional silencing of several tumor suppressors, and overexpression, amplification and somatic mutations have all been identified as mechanisms for the involvement of EZH2 in tumorigenesis. The new Transzyme EZH2 Assay kit is designed to accelerate efforts to develop selective EZH2 inhibitors using high throughput screening of small molecule libraries. The kit includes purified EZH2 from Reaction Biology, Histone H3 substrate, optimized buffer and the Transcreener EPIGEN Methyltransferase Assay reagents in a turn-key kit that has been pre-calibrated to produce HTSquality assay windows.
About BellBrook Labs. BellBrook Labs is dedicated to accelerating drug discovery and biological research by providing innovative high throughput screening solutions for enzymes and phenotypic assays. The company’s Transcreener® HTS enzyme assays, used by all of the major pharmaceutical companies, make it easy to screen thousands of different enzymes, including validated targets like kinases, as well as emerging targets like ATPases, GTPases, methyltransferases, and glycosyltransferases. The iuvo™ Microconduit Array technology and assay screening service are based on a line of unique microscale devices for miniaturization and automation of advanced cell models that are more representative of human physiology.