Brand  (β version)

PDB ID: 4R6V

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Ligands
Code Name Style Show Link
FI3 N-[4-({[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino}methyl)phenyl]propanamide PoSSuM
SO4 Sulfate ion PoSSuM
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Structure summary

Code : 4R6V   PDBj   RCSB PDB   PDBe
Header : Transferase/transferase inhibitor
Title : 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
Release Data : 2014-10-29
Compound :
mol_id molecule chains synonym
1 Fibroblast growth factor receptor 4 A FGFR-4
ec: 2.7.10.1
fragment: Tyrosine Kinase Domain of FGF receptor 4
mutation: R664E, V550L
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
gene: FGFR4, JTK2, TKF
Authors : Huang, Z., Mohammadi, M.
Keywords : Kinase Domain Fold, Cell Signaling, Phosphotransferase, Plasmamembrane, Transferase-transferase inhibitor complex
Exp. method : X-RAY DIFFRACTION ( 2.353 Å )
Citation :

Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.

Tan, L.,Wang, J.,Tanizaki, J.  et al.
(2014)  Proc.Natl.Acad.Sci.USA  111 : E4869 - E4877

PubMed: 25349422
DOI: 10.1073/pnas.1403438111

Reaction

Chain : A
UniProt : P22455 (FGFR4_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
ATP + L-tyrosyl-[protein] = ADP + H(+) + O-phospho-L-tyrosyl- [protein] 2.7.10.1 PROSITE-ProRule:PRU10028, PubMed:11433297, PubMed:17311277, PubMed:18480409, PubMed:18670643
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