› 6lud

X-ray diffraction
2.05Å resolution

Crystal Structure of EGFR(L858R/T790M/C797S) in complex with Osimertinib

Released:
DOI: 10.2210/pdb6lud/pdb
Model geometry
Fit model/data
PDB entry 6lud coloured by chain, front view.
PDB entry 6lud coloured by chain, side view.
PDB entry 6lud coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
CH7233163 Overcomes Osimertinib-Resistant EGFR-Del19/T790M/C797S Mutation.
Kashima K, Kawauchi H, Tanimura H, Tachibana Y, Chiba T, Torizawa T, Sakamoto H
Mol Cancer Ther 19 2288-2297 (2020)
PMID: 32943545

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: 37.33 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

Ligands and Environments

1 bound ligand:
Ligand YY3 1 x YY3
No modified residues

Experiments and Validation Details

wwPDB Validation report is not available for this entry.
X-ray source: PHOTON FACTORY BEAMLINE BL-17A
Spacegroup: I23
Unit cell:
a: 143.932Å b: 143.932Å c: 143.932Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.207 0.206 0.222
Expression system: Spodoptera frugiperda

Quick links

Citations

18 review citations

Acquired resistance to third-generation EGFR-TKIs and emerging next-generation EGFR inhibitors.
Du et al. (2021)
17 more

16 mentions without citation

Globally Approved EGFR Inhibitors: Insights into Their Syntheses, Target Kinases, Biological Activities, Receptor Interactions, and Metabolism.
Abourehab et al. (2021)
15 more