BellBrook Labs Launches Complete Methyltransferase Assay Solution to Accelerate Epigenetic Drug Discovery

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BellBrook Labs, an innovative developer of drug discovery tools, has combined their Transcreener HTS assay technology with Reaction Biology’s purified enzymes to provide a complete methyltransferase assay solution for inhibitor high throughput screening (HTS) and profiling. The new Transzyme Methyltransferase Assay Kits are designed to eliminate much of the costly assay development that has slowed the pursuit of promising epigenetic drug targets for cancer, metabolic disorders and other diseases.

Transzyme MT Assay Kits eliminate assay development.

Transzyme MT Assay Kits eliminate assay development.

“The Transzyme Kits can eliminate days or even weeks of assay development. An investigator should be able to start running dose response experiments with inhibitors the same day they receive a kit.”

Methyltransferase enzymes 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. There are more than 50 methyltransferases in humans, each with their own unique requirements and quirks. Weeks or even months can be spent on assay development, with time often wasted testing poorly characterized enzymes and conflicting published methods. To eliminate this hurdle, BellBrook Labs and Reaction Biology have partnered to develop a complete methyltransferase assay solution for inhibitor screening and profiling. The expanding line of Transzyme Methyltransferase Assays overcomes the assay problems by combining all of the required methyltransferase enzyme reaction components and BellBrook’s Transcreener detection reagents into well-defined kits that are validated to produce HTS-quality data. 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.

BellBrook introduced their Transcreener EPIGEN Methyltransferase assay last year to provide an HTS-proven assay method that could accommodate the diversity of methlytransferase enzymes and substrates. The development and validation of the assay was described in a joint publication with Novartis in January of 2012. The assays have been broadly adopted by the drug discovery community, but recurring customer problems with enzyme performance spurred development of a more complete Transzyme solution. In addition to the Transcreener EPIGEN detection reagents, the components of the kits include Reaction Biology’s high quality purified methyltransferases enzymes, peptide, protein, or DNA substrates, highly purified S-adenosylmethionine to drive the reactions and buffers optimized for each methlytransferase enzyme. By using following simple protocols, investigators should be able to generate HTS-quality assay data with virtually no time spent on assay development.

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. Visit BellBrook’s website for more information:

About Reaction Biology. Reaction Biology Corporation (“RBC”) is a premier provider of in vitro enzyme activity assays for HTS and profiling. Serving over 200 customers worldwide, RBC specializes in optimizing nanoliter scale assaying methods, allowing for high quality data with fast turnaround and economical pricing. RBC offers gold-standard radioisotope based assays in the Kinase, Methyltransferase, and HAT enzyme classes, as well as a full suite of HDAC/SIRT assays. RBC also now provides an expanding line of active, human recombinant HMTs, including some exclusive complexes. Compound libraries, custom assay development, discovery partnerships and cell-based assays are also part of RBC’s portfolio of services. Visit RBC’s website for more information:

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Robert Lowery
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