BellBrook Labs 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.

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 provide 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 the more complete Transzyme solution. In addition to the Transcreener EPIGEN detection reagents, each Transzyme kit includes one of Reaction Biology’s high quality purified methyltransferases enzymes, a corresponding peptide, protein, or DNA substrate, highly purified S-adenosylmethionine to drive the reactions and optimized enzyme buffers. By using following simple protocols, investigators should be able to generate HTS-quality assay data with virtually no time spent on assay development.