› 2qi8

X-ray diffraction
2.32Å resolution

Crystal structure of drug resistant SRC kinase domain

Released:
DOI: 10.2210/pdb2qi8/pdb
PDB entry 2qi8 coloured by chain, front view.
PDB entry 2qi8 coloured by chain, side view.
PDB entry 2qi8 coloured by chain, top view.
Source organism: Gallus gallus
Primary publication:
Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.
Michalczyk A, Klüter S, Rode HB, Simard JR, Grütter C, Rabiller M, Rauh D
Bioorg Med Chem 16 3482-8 (2008)
PMID: 18316192

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-132629 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Proto-oncogene tyrosine-protein kinase Src Chains: A, B
Molecule details ›
Chains: A, B
Length: 286 amino acids
Theoretical weight: 32.77 KDa
Source organism: Gallus gallus
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P00523 (Residues: 251-533; Coverage: 53%)
Gene name: SRC
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

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

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU MICROMAX-007
Spacegroup: P1
Unit cell:
a: 42Å b: 63.02Å c: 73.95Å
α: 78.78° β: 88.8° γ: 90.14°
R-values:
R R work R free
0.209 0.205 0.28
Expression system: Escherichia coli BL21(DE3)

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Citations

16 review citations

Lessons learned from lung cancer genomics: the emerging concept of individualized diagnostics and treatment.
Buettner et al. (2013)
15 more

1 mention without citation

How Electrostatic Coupling Enables Conformational Plasticity in a Tyrosine Kinase.
Tsai et al. (2019)