4QQ5

Crystal Structure of FGF Receptor (FGFR) 4 Kinase Harboring the V550L Gate-Keeper Mutation in Complex With FIIN-2, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR Kinase Gate-Keeper Mutations

Summary for 4QQ5

• Entry DOI: 10.2210/pdb4qq5/pdb
• Related: 4QQC 4QQJ 4QQT 4QRC
• Descriptor: Fibroblast growth factor receptor 4, N-(4-{[3-(3,5-dimethoxyphenyl)-7-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl}phenyl)propanamide (2 entities in total)
• Functional Keywords: kinase domain fold, cell signaling, phosphotransferase, plasmamembrane, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted. Isoform 3: Cytoplasm : P22455
• Total number of polymer chains: 1
• Total formula weight: 36810.34

Authors

Huang, Z.,Mohammadi, M. (deposition date: 2014-06-26, release date: 2014-10-29, Last modification date: 2023-09-20)

• Primary citation: Huang, Z.,Tan, L.,Wang, H.,Liu, Y.,Blais, S.,Deng, J.,Neubert, T.A.,Gray, N.S.,Li, X.,Mohammadi, M.; DFG-out Mode of Inhibition by an Irreversible Type-1 Inhibitor Capable of Overcoming Gate-Keeper Mutations in FGF Receptors.; Acs Chem.Biol., 10:299-309, 2015; PubMed: 25317566; DOI: 10.1021/cb500674s

Experimental method

X-RAY DIFFRACTION (2.203 Å)