Pryde, David C.; Middya, Sandip; Banerjee, Monali; Shrivastava, Ritesh; Basu, Sourav; Ghosh, Rajib; Yadav, Dharmendra B.; Surya, Arjun published the artcile< The discovery of potent small molecule activators of human STING>, Name: Ethyl 2-hydroxyacetate, the main research area is human STING activator preparation oxindole benzothiazine quinoline oxazine benzazepine; Cytokines; Immunotherapy; Interferon genes; STING.
The adaptor protein STING plays a major role in innate immune sensing of cytosolic nucleic acids, by triggering a robust interferon response. Despite the importance of this protein as a potential therapeutic target for serious unmet medical conditions including cancer and infectious disease there remains a paucity of STING ligands. Starting with a benzothiazinone series of weak STING activators (human EC50 ∼10μM) we identified several chemotypes with sub-micromolar STING activity across all the major protein polymorphs. An example compound I, based on an oxindole core structure, demonstrated robust on-target functional activation of STING (human EC50 185 nM) in immortalized and primary cells and a cytokine induction fingerprint consistent with STING activation. Our study has identified several related series of potent small mol. human STING activators with potential to be developed as immunomodulatory therapeutics.
European Journal of Medicinal Chemistry published new progress about Homo sapiens. 623-50-7 belongs to class esters-buliding-blocks, and the molecular formula is C4H8O3, Name: Ethyl 2-hydroxyacetate.
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