5V8O

Discovery of a high affinity inhibitor of cGAS

Summary for 5V8O

• Entry DOI: 10.2210/pdb5v8o/pdb
• Related: 5V8H 5V8J 5V8N
• Descriptor: Cyclic GMP-AMP synthase, ZINC ION, 5-phenyltetrazolo[1,5-a]pyrimidin-7-ol, ... (4 entities in total)
• Functional Keywords: cgas, sting, cgamp, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (Human)
• Cellular location: Cytoplasm, cytosol . Note=(Microbial infection) Upon infection with virulent M: Q8N884
• Total number of polymer chains: 2
• Total formula weight: 85580.22

Authors

Hall, J. (deposition date: 2017-03-22, release date: 2017-09-27, Last modification date: 2024-03-06)

• Primary citation: Hall, J.,Brault, A.,Vincent, F.,Weng, S.,Wang, H.,Dumlao, D.,Aulabaugh, A.,Aivazian, D.,Castro, D.,Chen, M.,Culp, J.,Dower, K.,Gardner, J.,Hawrylik, S.,Golenbock, D.,Hepworth, D.,Horn, M.,Jones, L.,Jones, P.,Latz, E.,Li, J.,Lin, L.L.,Lin, W.,Lin, D.,Lovering, F.,Niljanskul, N.,Nistler, R.,Pierce, B.,Plotnikova, O.,Schmitt, D.,Shanker, S.,Smith, J.,Snyder, W.,Subashi, T.,Trujillo, J.,Tyminski, E.,Wang, G.,Wong, J.,Lefker, B.,Dakin, L.,Leach, K.; Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay.; PLoS ONE, 12:e0184843-e0184843, 2017; PubMed: 28934246; DOI: 10.1371/journal.pone.0184843

Experimental method

X-RAY DIFFRACTION (3.1 Å)