› 2j6m

X-ray diffraction
3.1Å resolution

Crystal structure of EGFR kinase domain in complex with AEE788

Released:
DOI: 10.2210/pdb2j6m/pdb
PDB entry 2j6m coloured by chain, front view.
PDB entry 2j6m coloured by chain, side view.
PDB entry 2j6m coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.
Yun CH, Boggon TJ, Li Y, Woo MS, Greulich H, Meyerson M, Eck MJ
Cancer Cell 11 217-27 (2007)
PMID: 17349580

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 domain:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-132671 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Epidermal growth factor receptor Chain: A
Molecule details ›
Chain: A
Length: 327 amino acids
Theoretical weight: 37.3 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P00533 (Residues: 696-1022; Coverage: 28%)
Gene names: EGFR, ERBB, ERBB1, HER1
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

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

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 24-ID-C
Spacegroup: I23
Unit cell:
a: 145.309Å b: 145.309Å c: 145.309Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.202 0.199 0.249
Expression system: Spodoptera frugiperda

Quick links

Citations

141 review citations

EGFR antagonists in cancer treatment.
Ciardiello et al. (2008)
140 more

39 mentions without citation

Structure and clinical relevance of the epidermal growth factor receptor in human cancer.
Kumar et al. (2008)
38 more