› 5x2c

X-ray diffraction
2.05Å resolution

Crystal structure of EGFR 696-1022 T790M/V948R in complex with SKLB(5)

Released:
DOI: 10.2210/pdb5x2c/pdb
PDB entry 5x2c coloured by chain, front view.
PDB entry 5x2c coloured by chain, side view.
PDB entry 5x2c coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structural insights into drug development strategy targeting EGFR T790M/C797S.
Zhu SJ, Zhao P, Yang J, Ma R, Yan XE, Yang SY, Yang JW, Yun CH
Oncotarget 9 13652-13665 (2018)
PMID: 29568384

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 Chains: A, B
Molecule details ›
Chains: A, B
Length: 331 amino acids
Theoretical weight: 37.72 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

3 bound ligands:
Ligand EDO 10 x EDO
Ligand 7XR 2 x 7XR
Ligand CL 1 x CL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: BRUKER AXS MICROSTAR
Spacegroup: C2
Unit cell:
a: 155.758Å b: 72.451Å c: 76.159Å
α: 90° β: 113.41° γ: 90°
R-values:
R R work R free
0.175 0.175 0.202
Expression system: Spodoptera frugiperda

Quick links

Citations

3 review citations

Redox Regulation, Oxidative Stress, and Inflammation in Group 3 Pulmonary Hypertension.
Rudyk et al. (2021)
2 more

2 mentions without citation

C797S Resistance: The Undruggable EGFR Mutation in Non-Small Cell Lung Cancer?
Grabe et al. (2018)
1 more