Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice
oleh: 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
| Format: | Article |
|---|---|
| Diterbitkan: | Nature Portfolio 2017-09-01 |
Deskripsi
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.