› 3g6h

X-ray diffraction
2.35Å resolution

Src Thr338Ile inhibited in the DFG-Asp-Out conformation

Released:
DOI: 10.2210/pdb3g6h/pdb
PDB entry 3g6h coloured by chain, front view.
PDB entry 3g6h coloured by chain, side view.
PDB entry 3g6h coloured by chain, top view.
Source organism: Gallus gallus
Primary publication:
Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations.
Seeliger MA, Ranjitkar P, Kasap C, Shan Y, Shaw DE, Shah NP, Kuriyan J, Maly DJ
Cancer Res 69 2384-92 (2009)
PMID: 19276351

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
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 G6H 1 x G6H
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 8.2.1
Spacegroup: P1
Unit cell:
a: 41.938Å b: 63.344Å c: 74.179Å
α: 100.99° β: 89.39° γ: 90.2°
R-values:
R R work R free
0.228 0.225 0.283
Expression system: Escherichia coli

Quick links

Citations

17 review citations

ERK1/2 MAP kinases: structure, function, and regulation.
Roskoski R. (2012)
16 more

4 mentions without citation

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