› 3ug2

X-ray diffraction
2.5Å resolution

Crystal structure of the mutated EGFR kinase domain (G719S/T790M) in complex with gefitinib

Released:
DOI: 10.2210/pdb3ug2/pdb
PDB entry 3ug2 coloured by chain, front view.
PDB entry 3ug2 coloured by chain, side view.
PDB entry 3ug2 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structural basis for the altered drug sensitivities of non-small cell lung cancer-associated mutants of human epidermal growth factor receptor.
Yoshikawa S, Kukimoto-Niino M, Parker L, Handa N, Terada T, Fujimoto T, Terazawa Y, Wakiyama M, Sato M, Sano S, Kobayashi T, Tanaka T, Chen L, Liu ZJ, Wang BC, Shirouzu M, Kawa S, Semba K, Yamamoto T, Yokoyama S
Oncogene 32 27-38 (2013)
PMID: 22349823

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:
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-132701 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Epidermal growth factor receptor Chain: A
Molecule details ›
Chain: A
Length: 334 amino acids
Theoretical weight: 38.04 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P00533 (Residues: 695-1022; Coverage: 28%)
Gene names: EGFR, ERBB, ERBB1, HER1
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand IRE 1 x IRE
Ligand MES 1 x MES
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SPRING-8 BEAMLINE BL26B2
Spacegroup: I23
Unit cell:
a: 143.675Å b: 143.675Å c: 143.675Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.19 0.186 0.249
Expression system: Spodoptera frugiperda

Quick links

Citations

14 review citations

Fighting cancer drug resistance: Opportunities and challenges for mutation-specific EGFR inhibitors.
Juchum et al. (2015)
13 more

22 mentions without citation

Personalized cancer medicine: molecular diagnostics, predictive biomarkers, and drug resistance.
Gonzalez de Castro et al. (2013)
21 more