The cGAS–STING pathway as a therapeutic target in ... - Nature
Apr 8, 2021 · Insights into the structural and molecular biology of the cGAS–STING pathway have enabled the development of selective small-molecule inhibitors with the potential to target the...
Targeting STING with covalent small-molecule inhibitors
Jul 4, 2018 · In summary, our work uncovers a mechanism by which STING can be inhibited pharmacologically and demonstrates the potential of therapies that target STING for the treatment of autoinflammatory...
STING Agonists/Antagonists: Their Potential as Therapeutics and …
Inhibition of the cGAS/STING pathway can be achieved with cGAS (5) or STING (4) specific inhibitors (red triangle). This intervention might be relevant for many autoinflammatory diseases that show an increase in IFN type I response.
Drug developers switch gears to inhibit STING - Nature
Mar 4, 2019 · Several biotechs are exploring STING inhibitors as a means to control innate immunity and inflammation. Eli Lilly is the latest large pharma company to set its sights on cGAS–STING,...
Agonists and inhibitors of the STING pathway: Potential agents …
The STING pathway can be stimulated by cyclic dinucleotides (CDNs), leading to the type I interferons (IFN) production for immunotherapy for cancer or other diseases. However, the negative charges, hydrophilicity, and instability of CDNs have hindered their further applications.
STING inhibitors target the cyclic dinucleotide binding pocket
Structural optimization identified SN-011 as a potent STING inhibitor that impedes STING oligomerization, trafficking and activation in response to cytosolic DNA and markedly decreases STING-driven expression of type I IFNs and proinflammatory cytokines.
H151, a small molecule inhibitor of STING as a novel therapeutic …
H151, a novel STING inhibitor, attenuates the inflammatory response and reduces tissue injury and mortality in a murine model of intestinal I/R. H151 shows promise as a potential therapeutic in the treatment of this disease.
STING inhibitors target the cyclic dinucleotide binding pocket
Jun 15, 2021 · Cytosolic DNA activates cGAS (cytosolic DNA sensor cyclic AMP-GMP synthase)-STING (stimulator of interferon genes) signaling, which triggers interferon and inflammatory responses that help defend against microbial infection and cancer.
Targeting STING with covalent small-molecule inhibitors
Here we report the discovery and characterization of highly potent and selective small-molecule antagonists of the stimulator of interferon genes (STING) protein, which is a central signalling component of the intracellular DNA sensing pathway 1,2.
H-151 | STING-specific inhibitor - InvivoGen
InvivoGen provides high-quality H-151 (CAS 941987-60-6), a specific antagonist of both human and murine STING (stimulator of interferon genes). Our H-151 is functionally tested using cellular assays. H-151 suppresses type I Interferon production in autoimmune disease models.