Crystal Structure of FGF Receptor (FGFR) 4 Kinase Harboring the V550L Gate-Keeper Mutation in Complex with FIIN-3, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR kinase Gate-Keeper Mutations

Summary for 4R6V

Related4QQ5 4QQC 4QQT 4QRC 4QQJ
DescriptorFibroblast growth factor receptor 4, N-[4-({[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino}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 weight37059.35
Huang, Z.,Mohammadi, M. (deposition date: 2014-08-26, 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

Structure validation

RfreeClashscoreRamachandran outliersSidechain outliersRSRZ outliers0.236500.9%1.1%MetricValuePercentile RanksWorseBetterPercentile relative to all X-ray structuresPercentile relative to X-ray structures of similar resolution
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