4R6V
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
Entry DOI | 10.2210/pdb4r6v/pdb |
Related | 4QQ5 4QQC 4QQJ 4QQT 4QRC |
Descriptor | Fibroblast 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 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 | 37059.35 |
Authors | Huang, Z.,Mohammadi, M. (deposition date: 2014-08-26, release date: 2014-10-29, Last modification date: 2023-09-20) |
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 Cited by PubMed: 25349422DOI: 10.1073/pnas.1403438111 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.353 Å) |
Structure validation
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