Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice

Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice

Upon DNA binding cyclic GMP-AMP synthase (cGAS) produces a cyclic dinucleotide, which leads to the upregulation of inflammatory genes. Here the authors develop small molecule cGAS inhibitors, functionally characterize them and present the inhibitor and DNA bound cGAS crystal structures, which will f...

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Autores principales: Jessica Vincent, Carolina Adura, Pu Gao, Antonio Luz, Lodoe Lama, Yasutomi Asano, Rei Okamoto, Toshihiro Imaeda, Jumpei Aida, Katherine Rothamel, Tasos Gogakos, Joshua Steinberg, Seth Reasoner, Kazuyoshi Aso, Thomas Tuschl, Dinshaw J. Patel, J. Fraser Glickman, Manuel Ascano
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2017
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Science
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Acceso en línea:https://doaj.org/article/2885ccbed5fa465f9f9e037a1d7866c1
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Sumario:Upon DNA binding cyclic GMP-AMP synthase (cGAS) produces a cyclic dinucleotide, which leads to the upregulation of inflammatory genes. Here the authors develop small molecule cGAS inhibitors, functionally characterize them and present the inhibitor and DNA bound cGAS crystal structures, which will facilitate drug development.

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