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Keeping methyltransferases simple
FITCHBURG, Wis.—BellBrook Labs announced in mid-September that it was "undertaking a comprehensive effort" to validate purified human methyltransferases for robust, high-throughput screening-ready detection in BellBrook's recently developed Transcreener EPIGEN Methyltransferase Assay.
In this effort, the Madison-area company has been working with Malvern, Pa.-based Reaction Biology Corp., which is also the source of those purified human methyltransferases.
The team effort is aimed, the two companies say, "at accelerating public and private drug discovery initiatives targeting the epigenetic modifications that underlie a broad range of diseases, including cancer and autoimmune disorders."
The collaboration news was quickly followed by news at the beginning of October that the two companies had combined the Transcreener HTS assay technology with Reaction Biology's purified enzymes to provide "a complete methyltransferase assay solution for inhibitor high-throughput screening and profiling."
Discovery of new drugs that target methyltransferases has become a major initiative for many pharmaceutical and biotech companies because those enzymes are responsible for epigenetic modifications underlying a broad range of diseases; however, efforts to identify new molecules that disrupt the activity of aberrant methyltransferases have been slowed by the lack of robust high-throughput screening assays and high-quality, purified methyltransferase enzymes, the companies note. Further complicating the situation is the fact that each methyltransferase in humans requires a specialized set of conditions and components to produce activity.
"We launched the Transcreener EPIGEN back in September 2011, and a lot of customers and pharmas were evaluating it," recalls Robert Lowery, president and CEO of BellBrook Labs. "The assay worked great, but people have had trouble working with the methyltransferase enzymes—the enzymes are very complicated and they are challenging to use with kinases. So to help our customers, we pursued a strategy of looking at various commercial enzymes and we found Reaction Biology's to be very high quality. We began to evaluate specific enzymes of interest to make things easier for customers and that led to the concept of packaging their enzymes with the EPIGEN to give people a complete solution."
According to BellBrook, the Transcreener EPIGEN Methyltransferase Assay has universal applicability across the entire methyltransferase family. Meanwhile, Reaction Biology has produced more than 30 recombinant human methyltransferases to what the companies both call "the most stringent purity and activity requirements in the industry."
What BellBrook then did was to undertake a comprehensive effort to identify the optimal reaction conditions for each of Reaction Biology's methlytransferases in the EPIGEN Methyltransferase Assay. By taking much of the guesswork and upfront assay development out of methyltransferase screening and profiling, the companies say they had hoped their collaborative effort and resulting combined solution would accelerate the discovery of new drugs for diseases with an epigenetic basis and reduce the cost of developing assays for such purposes.
In truth, Lowery notes, the decision to launch a combined product line goes back to August, but the two companies wanted to make sure everything worked properly before officially announcing that. The two companies worked very well together, Lowery notes, and that led to a "flurry of activity" that resulted in a product line to announce just a couple months later.
"We found Reaction Biology to be really easy to work with, and they were open to the idea of collaborating and co-marketing right from the start," he says. "They are mostly service and screening and profiling, and we're making reagents, so there's really no competition between us and our goals align well. They do sell some products directly, but we will end up being a good distribution channel for them. Reaction Biology is an outstanding partner both from the scientific and business perspectives."