BellBrook Labs Launches Transcreener cGAS Activity Assay to Accelerate Drug Discovery

The newTranscreenercGAMPcGASAssay directly measures the productcGAMP, in acGASenzymatic reaction allowing researchers to screen vast compound libraries for modulators of the enzyme. The assay will be used to discover and develop new treatments for autoimmune diseases and cancer by strategically targeting thecGAS-STING pathway.


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Researchers atBellBrookLabs have developed a high throughput screening (HTS) compatible biochemical assay to discover and advance small molecule modulators for the target cyclic GMP-AMP synthase (cGAS).TheTranscreenercGAMPcGASAssay directly detects cyclic GMP-AMP (cGAMP), the product of acGASreaction, allowing researchers to monitorcGASactivity with simple, mix-and-read fluorescent detection.

The presence of DNA in the cytosol of eukaryotic cells is an indicator of infection or cellular damage, and it elicits a strong innate immune response.cGAStriggers this response to cytoplasmic DNA by producing the dinucleotide second messengercGAMP, which activates the stimulator of interferon genes (STING) receptor leading to a type I interferon response. Recent studies suggest thecGAS-STING pathway is a promising area for therapeutics targeting autoimmune disease and cancer.

TheTranscreenercGAMPcGASAssayis a competitive immunoassay that uses a highly specific antibody forcGAMPand a fluorescent tracer.cGAMPdisplaces the tracer from the antibody resulting in a robust fluorescent polarization (FP) readout. Along with basiccGASresearch including enzymology and regulation, the new assay ...

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