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BellBrook Labs Develops a TR-FRET Based Transcreener GTPase Assay

(PRWEB) July 16, 2014

BellBrook Labs announced the launch of a new Transcreener GDP Assay with a TR-FRET (time resolved Forster resonance energy transfer) readout, for sensitive detection of hundreds of enzymes of potential therapeutic interest including the large GTPase family as well as glycosyltransferase enzymes that use GDP-activated sugars; e.g., fucosyltransferases. These and related enzymes are being targeted for a diverse range of diseases, including cancers and anti-microbials, and robust high throughput assays are critical for these efforts. The TR-FRET detection mode is a highly preferred readout for HTS because it relies on a time-gated luminescence signal, making it resistant to prompt fluorescence screening compounds. Like the other Transcreener assays for ADP, AMP/GMP and UDP, the Transcreener GDP assay relies on direct immunodetection of the nucleotide product, and does not depend on coupling enzymes, which are prone to interference from screening compounds. It is the only HTS-compatible GTPase assay that uses direct GDP detection.

GTPases are a large family of enzymes that play diverse roles in normal and disease-related cell processes. It includes small GTPases in the Ras superfamily as well as the Galpha proteins that relay signals from G-protein coupled receptors. Though many GTPases are known to be intimately involved in disease pathways, they have yet to be exploited therapeutically, partially because they are difficult to incorporate into the high throughput screening assays used to identify lead drug molecules. The Transcreener GDP assay overcomes a longstanding problem in GTPase assays because it relies on direct detection of GDP rather than phosphate. Phosphate is a component of many biomolecules and commonly used reagents, and its ubiquitous presence in biological samples causes high background and false positives in the current GTPase enzyme assays. BellBrook’s assay detects GDP - a much more specific product of GTPase enzymes - eliminating the background problems associated with phosphate detection.

The new Transcreener GDP TR-FRET Assay produces a far-red, time-resolved Forester-resonance-energy-transfer (TR-FRET) signal that is less sensitive to interference from fluorescent compounds in comparison to other detection modes. Designed specifically for HTS and featuring a single addition mix-and-read format and room temperature reagent stability, the Transcreener GDP TR-FRET Assay is compatible with plate readers typically found in research labs as well as those used in HTS core facilities.

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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