› 4qrc

X-ray diffraction
1.9Å resolution

Crystal Structure of the Tyrosine Kinase Domain of FGF Receptor 4 in Complex with Ponatinib

Released:
DOI: 10.2210/pdb4qrc/pdb
PDB entry 4qrc coloured by chain, front view.
PDB entry 4qrc coloured by chain, side view.
PDB entry 4qrc coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors.
Huang Z, Tan L, Wang H, Liu Y, Blais S, Deng J, Neubert TA, Gray NS, Li X, Mohammadi M
ACS Chem Biol 10 299-309 (2015)
PMID: 25317566

Function and Biology Details

Reaction catalysed: 
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-149636 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Fibroblast growth factor receptor 4 Chain: A
Molecule details ›
Chain: A
Length: 323 amino acids
Theoretical weight: 36.13 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P22455 (Residues: 445-753; Coverage: 40%)
Gene names: FGFR4, JTK2, TKF
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand SO4 4 x SO4
Ligand 0LI 1 x 0LI
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: NSLS BEAMLINE X4C
Spacegroup: P21
Unit cell:
a: 42.722Å b: 61.593Å c: 60.311Å
α: 90° β: 97.94° γ: 90°
R-values:
R R work R free
0.173 0.17 0.207
Expression system: Escherichia coli

Quick links

Citations

4 review citations

Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors.
Dai et al. (2019)
3 more

9 mentions without citation

Signaling Pathway and Small-Molecule Drug Discovery of FGFR: A Comprehensive Review.
Zheng et al. (2022)
8 more