› 4gk3

X-ray diffraction
1.9Å resolution

Human EphA3 Kinase domain in complex with ligand 87

Released:
DOI: 10.2210/pdb4gk3/pdb
PDB entry 4gk3 coloured by chain, front view.
PDB entry 4gk3 coloured by chain, side view.
PDB entry 4gk3 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography.
Lafleur K, Dong J, Huang D, Caflisch A, Nevado C
J Med Chem 56 84-96 (2013)
PMID: 23253074

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-151400 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Ephrin type-A receptor 3 Chain: A
Molecule details ›
Chain: A
Length: 361 amino acids
Theoretical weight: 40.46 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P29320 (Residues: 606-947; Coverage: 36%)
Gene names: EPHA3, ETK, ETK1, HEK, TYRO4
Sequence domains:
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand L87 1 x L87
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: BRUKER AXS MICROSTAR
Spacegroup: P21
Unit cell:
a: 53.297Å b: 38.25Å c: 76.05Å
α: 90° β: 101.72° γ: 90°
R-values:
R R work R free
0.18 0.178 0.213
Expression system: Escherichia coli

Quick links

Citations

3 review citations

EphB4: A promising target for upper aerodigestive malignancies.
Salgia et al. (2018)
2 more

1 mention without citation

Structural Analysis of the Binding of Type I, I1/2, and II Inhibitors to Eph Tyrosine Kinases.
Dong et al. (2015)