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

Authors :
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
Source :
Nature Communications, Vol 10, Iss 1, Pp 1-14 (2019)
Publication Year :
2019
Publisher :
Nature Portfolio, 2019.

Abstract

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.

Subjects

Subjects :
Science

Details

Language :
English
ISSN :
20411723
Volume :
10
Issue :
1
Database :
Directory of Open Access Journals
Journal :
Nature Communications
Publication Type :
Academic Journal
Accession number :
edsdoj.6f06ae155ca2436dab39b0d693daf384
Document Type :
article
Full Text :
https://doi.org/10.1038/s41467-019-08620-4