› 3el8

X-ray diffraction
2.3Å resolution

Crystal structure of c-Src in complex with pyrazolopyrimidine 5

Released:
DOI: 10.2210/pdb3el8/pdb
PDB entry 3el8 coloured by chain, front view.
PDB entry 3el8 coloured by chain, side view.
PDB entry 3el8 coloured by chain, top view.
Source organism: Gallus gallus
Primary publication:
Small molecule recognition of c-Src via the Imatinib-binding conformation.
Dar AC, Lopez MS, Shokat KM
Chem Biol 15 1015-22 (2008)
PMID: 18940662

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
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 PD5 1 x PD5
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.3
Spacegroup: P1
Unit cell:
a: 42.375Å b: 63.693Å c: 73.792Å
α: 101.01° β: 90.25° γ: 90.12°
R-values:
R R work R free
0.218 0.218 0.262
Expression system: Escherichia coli BL21

Quick links

Citations

8 review citations

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

18 mentions without citation

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