4QQC

Crystal Structure of FGF Receptor (FGFR) 4 Kinase Domain in Complex with FIIN-2, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR Kinase Gate-Keeper Mutations

Summary for 4QQC

Related4R6V
DescriptorFibroblast 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, SULFATE ION, ... (4 entities in total)
Functional Keywordskinase domain fold, cell signaling, phosphotransferase, plasmamembrane, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological sourceHomo sapiens (human)
Cellular locationCell membrane; Single-pass type I membrane protein. Isoform 2: Secreted. Isoform 3: Cytoplasm  P22455
Total number of polymer chains1
Total molecular weight36892.38
Authors
Huang, Z.,Mohammadi, M. (deposition date: 2014-06-27, release date: 2014-10-29, Last modification date: 2014-11-26)
Primary citation
Tan, L.,Wang, J.,Tanizaki, J.,Huang, Z.,Aref, A.R.,Rusan, M.,Zhu, S.J.,Zhang, Y.,Ercan, D.,Liao, R.G.,Capelletti, M.,Zhou, W.,Hur, W.,Kim, N.,Sim, T.,Gaudet, S.,Barbie, D.A.,Yeh, J.R.,Yun, C.H.,Hammerman, P.S.,Mohammadi, M.,Janne, P.A.,Gray, N.S.
Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.
Proc.Natl.Acad.Sci.USA, 111:E4869-E4877, 2014
PubMed: 25349422 (PDB entries with the same primary citation)
DOI: 10.1073/pnas.1403438111
MImport into Mendeley
Experimental method
X-RAY DIFFRACTION (2.4 Å)
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Structure validation

RfreeClashscoreRamachandran outliersSidechain outliersRSRZ outliers0.214400.4%1.8%MetricValuePercentile RanksWorseBetterPercentile relative to all X-ray structuresPercentile relative to X-ray structures of similar resolution
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