BellBrook Labs Develops a TR-FRET Based Transcreener HTS Assay for Phosphodiesterases, Ligases, and Synthetases

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Scientists at BellBrook Labs developed a TR-FRET based version of the company’s Transcreener AMP2/GMP2 Assay, a high throughput screening assay that can be used for hundreds of enzymes, among them targets for cancer, cardiovascular diseases and infectious diseases. TR-FRET is the most preferred detection mode for HTS, and the availability of the new Transcreener assay will provide an attractive solution for scientists seeking a robust, HTS-proven solution for phosphodiesterase assays, ligase assays, and related assays.

BellBrook Labs announced the launch of a new Transcreener AMP2/GMP2 Assay with a TR-FRET (time resolved Forster resonance energy transfer) readout, for sensitive detection of hundreds of enzymes of potential therapeutic interest including ligases, synthetases, phosphodiesterases and sialyltransferases. These and related enzymes are being targeted for a diverse range of diseases, including cancer, cardiovascular disease and infectious diseases, and robust high throughput assays are critical for these efforts. The Transcreener AMP2/GMP2 Assay relies on a highly specific antibody that recognizes AMP, GMP and CMP, but not the cyclic or triphosphate forms of these nucleotides. First introduced in 2007 with a fluorescence polarization readout, the assay was improved in 2012 with a higher affinity antibody; the new TR-FRET detection format is the most preferred readout for HTS.

The Transcreener AMP2/GMP2 assay overcomes significant challenges in adapting phosphodiesterase assays, ligase assays, and synthetase assays to HTS by allowing direct detection of nanomolar quantities of nucleotide monophosphates in enzyme reactions without separating them from other reaction components; i.e., mix-and-read detection. It is the only AMP/GMP assay method that allows direct detection of unlabeled nucleotides without the use of coupling or reporter enzymes, which are prone to interference from screening compounds.

About BellBrook Labs. BellBrook Labs, LLC develops detection reagents and microfluidic devices that accelerate the discovery of more effective therapies for cancer and other debilitating diseases. Transcreener® is a universal, high throughput biochemical assay platform based on detection of nucleotides, including ADP, GDP, AMP, GMP and UDP which are formed by thousands of cellular enzymes, many of which catalyze the covalent regulatory reactions that are central to cell signaling and represent new opportunities for therapeutic intervention. The iuvo™ Microconduit Array technology and assay screening service is a line of unique microscale devices for miniaturization and automation of advanced cell models that are more representative of human physiology.

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Bob Lowery
BellBrook Labs
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