› 4c7t

X-ray diffraction
2.05Å resolution

Focal Adhesion Kinase catalytic domain in complex with a diarylamino- 1,3,5-triazine inhibitor

Released:
DOI: 10.2210/pdb4c7t/pdb
PDB entry 4c7t coloured by chain, front view.
PDB entry 4c7t coloured by chain, side view.
PDB entry 4c7t coloured by chain, top view.
Source organism: Gallus gallus
Primary publication:
Inhibition of both focal adhesion kinase and fibroblast growth factor receptor 2 pathways induces anti-tumor and anti-angiogenic activities.
Dao P, Jarray R, Smith N, Lepelletier Y, Le Coq J, Lietha D, Hadj-Slimane R, Herbeuval JP, Garbay C, Raynaud F, Chen H
Cancer Lett 348 88-99 (2014)
PMID: 24657306

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-169484 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Focal adhesion kinase 1 Chain: A
Molecule details ›
Chain: A
Length: 276 amino acids
Theoretical weight: 31.73 KDa
Source organism: Gallus gallus
Expression system: Trichoplusia ni
UniProt:
  • Canonical: Q00944 (Residues: 411-686; Coverage: 26%)
Gene names: FAK, FAK1, PTK2
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand 5RI 1 x 5RI
Ligand SO4 1 x SO4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ESRF BEAMLINE ID14-4
Spacegroup: P21
Unit cell:
a: 44.37Å b: 45.28Å c: 66.66Å
α: 90° β: 95.11° γ: 90°
R-values:
R R work R free
0.22 0.219 0.246
Expression system: Trichoplusia ni

Quick links

Citations

3 review citations

Role of microRNA-93 in regulation of angiogenesis.
Li et al. (2014)
2 more

3 mentions without citation

Drug Discovery Targeting Focal Adhesion Kinase (FAK) as a Promising Cancer Therapy.
Pang et al. (2021)
2 more