› 2oiq

X-ray diffraction
2.07Å resolution

Crystal Structure of chicken c-Src kinase domain in complex with the cancer drug imatinib.

Released:
DOI: 10.2210/pdb2oiq/pdb
PDB entry 2oiq coloured by chain, front view.
PDB entry 2oiq coloured by chain, side view.
PDB entry 2oiq coloured by chain, top view.
Source organism: Gallus gallus
Primary publication:
c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty.
Seeliger MA, Nagar B, Frank F, Cao X, Henderson MN, Kuriyan J
Structure 15 299-311 (2007)
PMID: 17355866

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: 32.73 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

2 bound ligands:
Ligand STI 1 x STI
Ligand GOL 2 x GOL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 8.2.1
Spacegroup: P1
Unit cell:
a: 42.078Å b: 63.373Å c: 74.474Å
α: 78.99° β: 89.12° γ: 90.1°
R-values:
R R work R free
0.232 0.227 0.263
Expression system: Escherichia coli BL21(DE3)

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Citations

17 review citations

The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling.
Dar et al. (2011)
16 more

30 mentions without citation

Mechanisms of drug resistance in kinases.
Barouch-Bentov et al. (2011)
29 more