4FLH

Crystal structure of human PI3K-gamma in complex with AMG511

Summary for 4FLH

• Entry DOI: 10.2210/pdb4flh/pdb
• Related: 4DK5 4F1S 4FJY 4FJZ
• Descriptor: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION, 4-(2-[(5-fluoro-6-methoxypyridin-3-yl)amino]-5-{(1R)-1-[4-(methylsulfonyl)piperazin-1-yl]ethyl}pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine, ... (4 entities in total)
• Functional Keywords: p110, phosphotransferase, cancer, p85, phosphorylation, transferase-inhibitor complex, transferase/inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Cytoplasm : P48736
• Total number of polymer chains: 1
• Total formula weight: 110725.89

Authors

Whittington, D.A.,Tang, J.,Yakowec, P. (deposition date: 2012-06-14, release date: 2012-08-29, Last modification date: 2024-02-28)

• Primary citation: Norman, M.H.,Andrews, K.L.,Bo, Y.Y.,Booker, S.K.,Caenepeel, S.,Cee, V.J.,D'Angelo, N.D.,Freeman, D.J.,Herberich, B.J.,Hong, F.T.,Jackson, C.L.,Jiang, J.,Lanman, B.A.,Liu, L.,McCarter, J.D.,Mullady, E.L.,Nishimura, N.,Pettus, L.H.,Reed, A.B.,Miguel, T.S.,Smith, A.L.,Stec, M.M.,Tadesse, S.,Tasker, A.,Aidasani, D.,Zhu, X.,Subramanian, R.,Tamayo, N.A.,Wang, L.,Whittington, D.A.,Wu, B.,Wu, T.,Wurz, R.P.,Yang, K.,Zalameda, L.,Zhang, N.,Hughes, P.E.; Selective Class I Phosphoinositide 3-Kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511.; J.Med.Chem., 55:7796-7816, 2012; PubMed: 22897589; DOI: 10.1021/jm300846z

Experimental method

X-RAY DIFFRACTION (2.6 Å)