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JUM 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
ZN Zinc ion
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Code : 6MJU   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE/TRANSFERASE INHIBITOR
Title : human cGAS catalytic domain bound with the inhibitor G108
Release Data : 2019-05-29
Compound :
mol_id molecule chains synonym
1 Cyclic GMP-AMP synthase A h-cGAS,2'3'-cGAMP synthase,Mab-21 domain-containing protein 1
ec: 2.7.7.86
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli BL21(DE3)  (taxid:469008)
gene: CGAS, C6orf150, MB21D1
expression_system_strain: BL21(DE3)
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.
Keywords : human cGAS, DNA sensor, IMMUNE SYSTEM, TRANSFERASE-TRANSFERASE INHIBITOR complex
Exp. method : X-RAY DIFFRACTION ( 2.450 Å )
Citation :

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

Lama, L.,Adura, C.,Xie, W.  et al.
(2019)  Nat Commun  10 : 2261 - 2261

PubMed: 31113940
DOI: 10.1038/s41467-019-08620-4

Chain : A
UniProt : Q8N884 (CGAS_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
ATP + GTP = 2',3'-cGAMP + 2 diphosphate 2.7.7.86 PubMed:23258413, PubMed:23707061, PubMed:23722159, PubMed:25131990, PubMed:28934246, PubMed:29976794, PubMed:30799039, PubMed:31142647, PubMed:32814054, PubMed:33542149
left-to-right PubMed:23258413, PubMed:28934246