› 4qqj

X-ray diffraction
1.68Å resolution

Crystal Structure of FGF Receptor (FGFR) 4 Kinase Domain Harboring the V550L Gate-Keeper Mutation

Released:
DOI: 10.2210/pdb4qqj/pdb
PDB entry 4qqj coloured by chain, front view.
PDB entry 4qqj coloured by chain, side view.
PDB entry 4qqj 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: 36.14 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

1 bound ligand:
Ligand SO4 2 x SO4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: NSLS BEAMLINE X4C
Spacegroup: P21
Unit cell:
a: 42.671Å b: 61.472Å c: 61.819Å
α: 90° β: 99.43° γ: 90°
R-values:
R R work R free
0.195 0.193 0.22
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

2 mentions without citation

DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors.
Huang et al. (2015)
1 more