Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression

Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression

Cyclic GMP-AMP synthase (cGAS) is involved in the modulation of inflammatory responses. Here, the authors present small-molecule inhibitors of human cGAS, characterize their interaction with the protein, and show that the compounds are active in interferon-producing cells including primary human mac...

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Auteurs principaux: Lodoe Lama, Carolina Adura, Wei Xie, Daisuke Tomita, Taku Kamei, Vitaly Kuryavyi, Tasos Gogakos, Joshua I. Steinberg, Michael Miller, Lavoisier Ramos-Espiritu, Yasutomi Asano, Shogo Hashizume, Jumpei Aida, Toshihiro Imaeda, Rei Okamoto, Andy J. Jennings, Mayako Michino, Takanobu Kuroita, Andrew Stamford, Pu Gao, Peter Meinke, J. Fraser Glickman, Dinshaw J. Patel, Thomas Tuschl
Format: article
Langue:EN
Publié: Nature Portfolio 2019
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Science
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Accès en ligne:https://doaj.org/article/6f06ae155ca2436dab39b0d693daf384
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Résumé:Cyclic GMP-AMP synthase (cGAS) is involved in the modulation of inflammatory responses. Here, the authors present small-molecule inhibitors of human cGAS, characterize their interaction with the protein, and show that the compounds are active in interferon-producing cells including primary human macrophages.

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