6MJU

human cGAS catalytic domain bound with the inhibitor G108

Summary for 6MJU

• Entry DOI: 10.2210/pdb6mju/pdb
• Descriptor: Cyclic GMP-AMP synthase, 1-[6,7-dichloro-9-(1H-pyrazol-4-yl)-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indol-2-yl]-2-hydroxyethan-1-one, ZINC ION, ... (4 entities in total)
• Functional Keywords: human cgas, dna sensor, immune system, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 43916.67

Authors

Lama, L.,Adura, C.,Xie, W.,Tomita, D.,Kamei, T.,Kuryavyi, V.,Gogakos, T.,Steinberg, J.I.,Miller, M.,Ramos-Espiritu, L.,Asano, Y.,Hashizume, S.,Aida, J.,Imaeda, T.,Okamoto, R.,Jennings, A.J.,Michinom, M.,Kuroita, T.,Stamford, A.,Gao, P.,Meinke, P.,Glickman, J.F.,Patel, D.J.,Tuschl, T. (deposition date: 2018-09-22, release date: 2019-05-29, Last modification date: 2024-03-13)

• Primary citation: Lama, L.,Adura, C.,Xie, W.,Tomita, D.,Kamei, T.,Kuryavyi, V.,Gogakos, T.,Steinberg, J.I.,Miller, M.,Ramos-Espiritu, L.,Asano, Y.,Hashizume, S.,Aida, J.,Imaeda, T.,Okamoto, R.,Jennings, A.J.,Michino, M.,Kuroita, T.,Stamford, A.,Gao, P.,Meinke, P.,Glickman, J.F.,Patel, D.J.,Tuschl, T.; Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression.; Nat Commun, 10:2261-2261, 2019; PubMed: 31113940; DOI: 10.1038/s41467-019-08620-4

Experimental method

X-RAY DIFFRACTION (2.45 Å)