• Assay Selection Tool

BellBrook Labs

  • Products
    • Transcreener® HTS Assay Kits
      • Transcreener® ADP² Kinase Assay Kits
        • Transcreener® ADP2 Assay Kit – FP Readout
        • Transcreener® ADP2 Assay Kit – FI Readout
        • Transcreener® ADP2 Assay Kit – TR-FRET Readout
      • Transcreener® ADO CD73 Assay Kit
      • Transcreener® AMP²/GMP² Phosphodiesterase Assay Kits
        • Transcreener® AMP2/GMP2 FP Assay
        • Transcreener® AMP2/GMP2 Assay Kit – TR-FRET Readout
      • Transcreener® cGAMP cGAS Assay Kits
        • Transcreener® cGAMP Assay Kit – FP Readout
        • Transcreener® cGAMP Assay Kit – TR-FRET Readout
      • Transcreener dAMP Exonuclease Assay Kit
      • Transcreener® EPIGEN SAH Methyltransferase Assay Kit
      • Transcreener® GDP GTPase Assay Kits
        • Transcreener® GDP Assay Kit – FP Readout
        • Transcreener® GDP Assay Kit – FI Readout
        • Transcreener® GDP Assay Kit – TR-FRET Readout
      • Transcreener® UDP² Glycosyltransferase Assay Kits
        • Transcreener® UDP2 Assay Kit – FP Readout
        • Transcreener® UDP2 Assay Kit – FI Readout
        • Transcreener® UDP2 Assay Kit – TR-FRET Readout
      • Transcreener® 2-5A OAS Assay Kit
    • AptaFluor® HTS Assay Kits
      • AptaFluor® SAH Methyltransferase Assay Kit
    • Enzyme Assay Systems
      • TREX1 Assay System
    • Recombinant Enzymes
      • Human cGAS Enzyme
      • Mouse cGAS Enzyme
      • Human DDX3 Enzyme
      • Human OAS1 Enzyme
      • Human TREX1 Enzyme
    • Assay Plates
    • Ordering Information
  • Services
    • Assay Development Services
    • Lead Discovery Services
    • CD38 Assay Services
    • GTPase Profiling Services
    • ATPase Profiling Services
  • Assays by Target
    • Kinase Assays
      • ADK Assays – Application
      • AMPK Assays – Application
      • IKK-beta Assays – Application
      • IRAK4 Assays – Application
      • JAK1 Assays – Application
      • JAK3 Assays – Application
      • MAPK8 Assays – Application
      • PKR Assays – Application
      • RIPK1 Assays – Application
      • RIPK2 Assays – Application
      • TBK1 Assays – Application
    • GTPase Assays
      • GAP Assays – Application
      • GEF Assays – Application
      • KRAS Assays – Application
      • HRAS Assays – Application
      • NRAS Assays – Application
      • RRAS Assays – Application
      • Rac1 Assays – Application
      • RhoA Assays – Application
      • RhoC Assays – Application
      • Cdc42 Assays – Application
      • Ran Assays – Application
    • Methyltransferase Assays
      • EZH2 Assays – Application
      • G9a Assays – Application
      • SET7/9 Assays – Application
      • SET8 Assays – Application
      • PRMT1 Assays – Application
      • PRMT3 Assays – Application
      • PRMT4 Assay – Application
    • STING Pathway Assays
      • cGAS Assay Kits
      • ENPP1 Assays – Application
      • TREX1 Assay System
      • IKK-beta Assays – Application
      • TBK1 Assays – Application
    • Nucleotidase Assays
      • CD38 Assay Services
      • CD39 Assays – Application
      • CD73 Activity Assay Kits
    • Helicase / ATPase Assays
      • DDX3 Assays – Application
      • NSP13 Assays – Application
      • P97 Assays – Application
    • Glycosyltransferase Assays
      • Toxin B Assays – Application
      • GALNT2 Assays – Application
      • GALNT3 Assays – Application
      • BGalT1 Assays – Application
    • Phosphodiesterase Assays
      • PDE3 Assays – Application
      • PDE4 Assays – Application
      • PDE5 Assays – Application
      • PDE7 Assays – Application
    • Ligase and Synthetase Assays
      • SUMO E1 Assays – Application
      • Acyl CoA Synthetase Assays – Application
      • S-Acetyl CoA Synthetase Assays – Application
    • Exonuclease Assays
      • TREX1 Assay System
    • OAS Assays
      • OAS1 Assay Kits
    • Other Enzyme Assays
      • NUDT5 Assays – Application
  • Resources
    • Technical Manuals
    • Transcreener® Assays – Instrument Compatibility
    • Application Notes
    • Posters and Presentations
    • Publications
    • Transcreener® FAQ’s
    • Guides
      • Residence Time Guide
      • Hit Prioritization Guide
      • Kinases in Innate Immunity
  • Company
    • President’s Message
    • International Distributors
    • Careers
    • Downloads
    • Contact Us
  • Blog
  • MY CART
    No products in cart.

NIH Awards BellBrook Labs Phase II Grant to Develop HTS Assays Targeting the cGAS-STING Pathway for Autoimmune Diseases and Cancer

by Bellbrook Labs / Tuesday, 22 May 2018 / Published in Company, Emerging Targets, News
Autoimmune Disease News

The National Institutes of General Medical Sciences (NIGMS) recently awarded BellBrook Labs a $1 million phase II Small Business Innovative Research (SBIR) grant to develop new assays to detect cyclic GMP-AMP (cGAMP) levels in biological samples. The assays will be used to discover, develop, and monitor new treatments for autoimmune diseases and cancer by targeting the cGAS-STING pathway.

Madison, WI – May 2018 – BellBrook Labs has been awarded a $1 million phase II SBIR grant by the National Institutes of General Medical Sciences to develop assays to detect cGAMP in biological samples.  cGAMP is produced by the enzyme cyclic GMP-AMP synthase (cGAS), which acts as a trigger for activation of an innate immune response to cytoplasmic DNA. The new assays will provide direct in-well detection of cGAMP in cell lysates to enable basic cellular research and screening for modulators of the cGAS-STING pathway.  Additionally, detection of cGAMP in human tissue samples will allow investigation of cGAMP as a biomarker for autoimmune disease status and drug efficacy.

Detection of foreign nucleic acids is an essential first line of defense in the immune response to microbial pathogens. However, aberrant induction of type I interferons (IFN) by self-nucleic acids causes devastating autoimmune diseases such as Aicardi–Goutieres Syndrome (AGS) and systemic lupus erythematosus (SLE).  Production of the unique cyclic dinucleotide, cGAMP, by the cytosolic DNA sensor, cGAS is a key molecular trigger for nucleic acid-driven type I IFN induction. The cGAS apoenzyme is enzymatically inactive; binding of non-specific dsDNA induces a transition to an active conformation that catalyzes the formation of cGAMP from ATP and GTP. cGAMP binds to the STING (stimulator of interferon genes) receptor to initiate the signaling for induction of type I IFNs. Thus, the cGAS enzyme senses the primary signal for a type I IFN response and amplifies it in the form of a second messenger. Knockout studies in animal models have clearly indicated that inhibiting cGAS is a promising approach for therapeutic intervention in monogenic type I interferonopathies such as AGS and, by extension, complex diseases such as SLE.

In phase, I, researchers at BellBrook Labs successfully developed an HTS compatible biochemical assay to discover and develop small molecule modulators targeting the enzyme cGAS. Cellular assays will be used to test the activity of cGAS modulators identified in biochemical screens and to allow cellular screening for compounds that activate or inhibit cGAS via diverse mechanisms. Assays for detecting cGAMP in cell and tissue samples would provide a simple, direct way to monitor the action of lead molecules targeting cGAS, and eventually for identification of responders in clinical studies. For example, Lupus patients with high levels of cGAMP could be candidates for cGAS inhibitors.

Combining results from biochemical screening with accurate validation in cellular assays will accelerate the discovery of potent modulators of the enzyme. The availability of assays to measure cGAMP in human samples will facilitate the development of personalized therapeutic approaches for debilitating autoimmune diseases.

Read about the Transcreener cGAMP cGAS Assay

Research reported in this publication was supported by the National Institute Of General Medical Sciences of the National Institutes of Health under Award Number R44GM123833. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health.

Tagged under: Transcreener cGAMP cGAS Assay

What you can read next

BELLBROOK LABS RECEIVES PATENT FOR TRANSCREENER ASSAY METHOD TO SCREEN GROUP TRANSFER REACTIONS
New Publication: TR-FRET Assay for UDP-Glycosyltransferases
BellBrook Labs Develops a More Cost Effective Solution for Screening Phosphodiesterases, Ligases, and Synthetases

Categories

  • Company
  • Emerging Targets
  • Epigenetics
  • HTS Assays
  • Innate Immunity
  • Neurodegenerative Diseases
  • News
  • Products
  • Resources
  • Success Stories
  • Uncategorized

Recent Posts

  • PARP1 as a Hero vs Villain

    Is PARP1 a Hero or Villain?

    Not counting histones, PARP1 [Poly(ADP-ribose) ...
  • Ongoing Puzzle of c-SRC in Cancer Treatment

    Advancements in The Ongoing Puzzle to Understand c-SRC

    Nearly a half-century ago, sequences from the R...
  • SLAS 2023 Conference Exhibitor Announcement

    SLAS 2023 – HTS Assays and Discovery Services

    BellBrook Labs will exhibit and present posters...
  • BTK's Involved in Systemic lupus erythematosus

    The Challenging Search for BTK Inhibitors

    Bruton’s Tyrosine Kinase (BTK) is a 76kDa...
  • SARM1 Causes Axonal Death

    SARM1 Forefronts Research into Major Neurological Diseases

    SARM1 [Sterile alpha & toll/interleukin rec...

Archives

BellBrook Labs
5500 Nobel Drive, Suite 230
Madison, Wisconsin 53711 USA
(608) 443-2400

info@bellbrooklabs.com

 Copyright © 2023 BellBrook Labs | All Rights Reserved | Privacy Policy | Terms of Use | FCOI | Sitemap

TOP