5KAE

Crystal structure of human PI3K-gamma in complex with quinoline-containing inhibitor 5g

Summary for 5KAE

• Entry DOI: 10.2210/pdb5kae/pdb
• Descriptor: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION, 4-azanyl-6-[[(1~{S})-1-(6-fluoranyl-3-phenyl-4-piperazin-1-ylcarbonyl-quinolin-2-yl)ethyl]amino]pyrimidine-5-carbonitrile, ... (4 entities in total)
• Functional Keywords: phosphotransferase, inhibitor, inflammatory disease, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (Human)
• Cellular location: Cytoplasm : P48736
• Total number of polymer chains: 1
• Total formula weight: 110551.73

Authors

Whittington, D.A.,Tang, J.,Yakowec, P. (deposition date: 2016-06-01, release date: 2017-06-21, Last modification date: 2023-09-27)

• Primary citation: Gonzalez-Lopez de Turiso, F.,Hao, X.,Shin, Y.,Bui, M.,Campuzano, I.,Cardozo, M.,Dunn, M.C.,Duquette, J.,Fisher, B.,Foti, R.S.,Henne, K.,He, X.,Hu, Y.-L.,Kelly, R.C.,Johnson, M.G.,Lucas, B.S.,McCarter, J.,McGee, L.R.,Medina, J.C.,Metz, D.,San Miguel, T.,Mohn, D.,Tran, T.,Vissinga, C.,Wannberg, S.,Whittington, D.A.,Whoriskey, J.,Yu, G.,Zalameda, L.,Zhang, X.,Cushing, T.D.; Discovery and in vivo evaluation of the potent and selective PI3K-delta inhibitors AM-0687 and AM-1430; To Be Published,

Experimental method

X-RAY DIFFRACTION (2.65 Å)