› 4feq

X-ray diffraction
2.2Å resolution

Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)

Released:
DOI: 10.2210/pdb4feq/pdb
PDB entry 4feq coloured by chain, front view.
PDB entry 4feq coloured by chain, side view.
PDB entry 4feq coloured by chain, top view.
Source organism: Mus musculus
Primary publication:
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
Powell NA, Hoffman JK, Ciske FL, Kaufman MD, Kohrt JT, Quin J, Sheehan DJ, Delaney A, Baxi SM, Catana C, McConnell P, Ohren J, Perrin LA, Edmunds JJ
Bioorg Med Chem Lett 23 1046-50 (2013)
PMID: 23312472

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-157207 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Tyrosine-protein kinase receptor TYRO3 Chain: A
Molecule details ›
Chain: A
Length: 323 amino acids
Theoretical weight: 36.77 KDa
Source organism: Mus musculus
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P55144 (Residues: 485-800; Coverage: 37%)
Gene names: Dtk, Rse, Tif, Tyro3
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand 0T8 1 x 0T8
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 17-ID
Spacegroup: P21
Unit cell:
a: 47.778Å b: 57.157Å c: 60.676Å
α: 90° β: 100.69° γ: 90°
R-values:
R R work R free
0.278 0.275 0.327
Expression system: Spodoptera frugiperda

Quick links

Citations

4 review citations

The TAM family: phosphatidylserine sensing receptor tyrosine kinases gone awry in cancer.
Graham et al. (2014)
3 more

1 mention without citation

Structural elucidation of the DFG-Asp in and DFG-Asp out states of TAM kinases and insight into the selectivity of their inhibitors.
Messoussi et al. (2014)