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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Acceso en línea:https://doaj.org/article/2885ccbed5fa465f9f9e037a1d7866c1
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spelling oai:doaj.org-article:2885ccbed5fa465f9f9e037a1d7866c12021-12-02T14:40:35ZSmall molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice10.1038/s41467-017-00833-92041-1723https://doaj.org/article/2885ccbed5fa465f9f9e037a1d7866c12017-09-01T00:00:00Zhttps://doi.org/10.1038/s41467-017-00833-9https://doaj.org/toc/2041-1723Upon 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.Jessica VincentCarolina AduraPu GaoAntonio LuzLodoe LamaYasutomi AsanoRei OkamotoToshihiro ImaedaJumpei AidaKatherine RothamelTasos GogakosJoshua SteinbergSeth ReasonerKazuyoshi AsoThomas TuschlDinshaw J. PatelJ. Fraser GlickmanManuel AscanoNature PortfolioarticleScienceQENNature Communications, Vol 8, Iss 1, Pp 1-13 (2017)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
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
Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice
description 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.
format article
author 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
author_facet 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
author_sort Jessica Vincent
title Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice
title_short Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice
title_full Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice
title_fullStr Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice
title_full_unstemmed Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice
title_sort small molecule inhibition of cgas reduces interferon expression in primary macrophages from autoimmune mice
publisher Nature Portfolio
publishDate 2017
url https://doaj.org/article/2885ccbed5fa465f9f9e037a1d7866c1
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