3L08

Structure of Pi3K gamma with a potent inhibitor: GSK2126458

Summary for 3L08

• Entry DOI: 10.2210/pdb3l08/pdb
• Descriptor: Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION, 2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl]benzenesulfonamide, ... (4 entities in total)
• Functional Keywords: pi3k gamma, lipid kinase, phosphoinositide, inhibitor, gsk2126458, signaling, kinase, atp-binding, nucleotide-binding, transferase
• Biological source: Homo sapiens (human)
• Cellular location: Cytoplasm : P48736
• Total number of polymer chains: 1
• Total formula weight: 111424.72

Authors

Elkins, P.A.,Marrero, E.M. (deposition date: 2009-12-09, release date: 2010-06-23, Last modification date: 2024-04-03)

• Primary citation: Knight, S.D.,Adams, N.D.,Burgess, J.L.,Chaudhari, A.M.,Darcy, M.G.,Donatelli, C.A.,Luengo, J.I.,Newlander, K.A.,Parrish, C.A.,Ridgers, L.H.,Sarpong, M.A.,Schmidt, S.J.,Van Aller, G.S.,Carson, J.D.,Diamond, M.A.,Elkins, P.A.,Gardiner, C.M.,Garver, E.,Gilbert, S.A.,Gontarek, R.R.,Jackson, J.R.,Kershner, K.L.,Luo, L.,Raha, K.,Sherk, C.S.,Sung, C.M.,Sutton, D.,Tummino, P.J.,Wegrzyn, R.J.,Auger, K.R.,Dhanak, D.; Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.; ACS Med Chem Lett, 1:39-43, 2010; PubMed: 24900173; DOI: 10.1021/ml900028r

Experimental method

X-RAY DIFFRACTION (2.7 Å)