› 4zau

X-ray diffraction
2.8Å resolution

AZD9291 complex with wild type EGFR

Released:
DOI: 10.2210/pdb4zau/pdb
PDB entry 4zau coloured by chain, front view.
PDB entry 4zau coloured by chain, side view.
PDB entry 4zau coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed.
Yosaatmadja Y, Silva S, Dickson JM, Patterson AV, Smaill JB, Flanagan JU, McKeage MJ, Squire CJ
J Struct Biol 192 539-544 (2015)
PMID: 26522274

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-132671 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Epidermal growth factor receptor Chain: A
Molecule details ›
Chain: A
Length: 330 amino acids
Theoretical weight: 37.56 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 YY3 1 x YY3
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU MICROMAX-007 HF
Spacegroup: I23
Unit cell:
a: 144.886Å b: 144.886Å c: 144.886Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.196 0.193 0.244
Expression system: Spodoptera frugiperda

Quick links

Citations

20 review citations

Rare epidermal growth factor receptor (EGFR) mutations in non-small cell lung cancer.
Harrison et al. (2020)
19 more

48 mentions without citation

Covalent Inhibition in Drug Discovery.
Ghosh et al. (2019)
47 more