› 5nud

X-ray diffraction
2.5Å resolution

FIBROBLAST GROWTH FACTOR RECEPTOR 4 KINASE DOMAIN (449-753) IN COMPLEX WITH IRREVERSIBLE LIGAND CGA159527

Released:
DOI: 10.2210/pdb5nud/pdb
PDB entry 5nud coloured by chain, front view.
PDB entry 5nud coloured by chain, side view.
PDB entry 5nud coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region.
Fairhurst RA, Knoepfel T, Leblanc C, Buschmann N, Gaul C, Blank J, Galuba I, Trappe J, Zou C, Voshol J, Genick C, Brunet-Lefeuvre P, Bitsch F, Graus-Porta D, Furet P
Medchemcomm 8 1604-1613 (2017)
PMID: 30108871

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 Chains: A, B
Molecule details ›
Chains: A, B
Length: 307 amino acids
Theoretical weight: 34.37 KDa
Source organism: Homo sapiens
UniProt:
  • Canonical: P22455 (Residues: 449-753; Coverage: 39%)
Gene names: FGFR4, JTK2, TKF
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand 99K 2 x 99K
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SLS BEAMLINE X10SA
Spacegroup: C2221
Unit cell:
a: 82.899Å b: 87.054Å c: 182.052Å
α: 90° β: 90° γ: 90°

Quick links

Citations

1 review citation

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

3 mentions without citation

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