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ACS Chem Biol. 2020 Jan 27. doi: 10.1021/acschembio.9b00810. [Epub ahead of print]

Small-Molecule Antagonists of the RIG-I Innate Immune Receptor.

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Inflammatix, Inc , Burlingame , California 94010 , United States.
Department of Molecular, Cellular and Developmental Biology , Yale University , New Haven , Connecticut 06520 , United States.
Howard Hughes Medical Institute , New Haven , Connecticut 06520 , United States.


The RIG-I receptor plays a key role in the vertebrate innate immune system, where it functions as a sensor for detecting infection by RNA viruses. Although agonists of RIG-I show great potential as antitumor and antimicrobial therapies, antagonists of RIG-I remain undeveloped, despite the role of RIG-I hyperstimulation in a range of diseases, including COPD and autoimmune disorders. There is now a wealth of information on RIG-I structure, enzymatic function, and signaling mechanism that can drive new drug design strategies. Here, we used the enzymatic activity of RIG-I to develop assays for high-throughput screening, SAR, and downstream optimization of RIG-I antagonists. Using this approach, we have developed potent RIG-I antagonists that interact directly with the receptor and which inhibit RIG-I signaling and interferon response in living cells.


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