› 6jpe

X-ray diffraction
1.6Å resolution

Crystal structure of FGFR4 kinase domain with irreversible inhibitor 1

Released:
DOI: 10.2210/pdb6jpe/pdb
PDB entry 6jpe coloured by chain, front view.
PDB entry 6jpe coloured by chain, side view.
PDB entry 6jpe coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Development of a Potent and Specific FGFR4 Inhibitor for the Treatment of Hepatocellular Carcinoma.
Rezende Miranda R, Fu Y, Chen X, Perino J, Cao P, Carpten J, Chen Y, Zhang C
J Med Chem 63 11484-11497 (2020)
PMID: 33030342

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: 311 amino acids
Theoretical weight: 34.66 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

Ligands and Environments

2 bound ligands:
Ligand BYU 1 x BYU
Ligand SO4 2 x SO4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SSRF BEAMLINE BL19U1
Spacegroup: P21
Unit cell:
a: 42.502Å b: 61.126Å c: 61.412Å
α: 90° β: 99.1° γ: 90°
R-values:
R R work R free
0.154 0.152 0.183
Expression system: Escherichia coli

Quick links

Citations

4 review citations

Targeting MCL-1 in cancer: current status and perspectives.
Wang et al. (2021)
3 more

2 mentions without citation

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