› 4i1z

X-ray diffraction
3Å resolution

Crystal structure of the monomeric (V948R) form of the gefitinib/erlotinib resistant EGFR kinase domain L858R+T790M

Released:
DOI: 10.2210/pdb4i1z/pdb
PDB entry 4i1z coloured by chain, front view.
PDB entry 4i1z coloured by chain, side view.
PDB entry 4i1z coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Insights into the aberrant activity of mutant EGFR kinase domain and drug recognition.
Gajiwala KS, Feng J, Ferre R, Ryan K, Brodsky O, Weinrich S, Kath JC, Stewart A
Structure 21 209-19 (2013)
PMID: 23273428

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: 329 amino acids
Theoretical weight: 37.58 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

No bound ligands
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 17-ID
Spacegroup: P3221
Unit cell:
a: 107.603Å b: 107.603Å c: 104.025Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.189 0.187 0.227
Expression system: Spodoptera frugiperda

Quick links

Citations

17 review citations

FDA-approved small-molecule kinase inhibitors.
Wu et al. (2015)
16 more

4 mentions without citation

Untangling Dual-Targeting Therapeutic Mechanism of Epidermal Growth Factor Receptor (EGFR) Based on Reversed Allosteric Communication.
Qiu et al. (2021)
3 more