› 2qlq

X-ray diffraction
2.33Å resolution

Crystal structure of SRC kinase domain with covalent inhibitor RL3

Released:
DOI: 10.2210/pdb2qlq/pdb
PDB entry 2qlq coloured by chain, front view.
PDB entry 2qlq coloured by chain, side view.
PDB entry 2qlq 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: 32.74 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 SR2 3 x SR2
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU MICROMAX-007
Spacegroup: P1
Unit cell:
a: 41.94Å b: 63.53Å c: 74.5Å
α: 78.28° β: 90.37° γ: 89.45°
R-values:
R R work R free
0.215 0.212 0.267
Expression system: Escherichia coli BL21(DE3)

Quick links

Citations

15 review citations

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

1 mention without citation

Three-Dimensional Interactions Analysis of the Anticancer Target c-Src Kinase with Its Inhibitors.
Jha et al. (2020)