› 6cz4

X-ray diffraction
1.5Å resolution

Structure of the PTK6 kinase domain bound to a type II inhibitor 2-{[(3R,4S)-3-fluoro-1-{[4-(trifluoromethoxy)phenyl]acetyl}piperidin-4-yl]oxy}-5-(1-methyl-1H-imidazol-4-yl)pyridine-3-carboxamide

Released:
DOI: 10.2210/pdb6cz4/pdb
PDB entry 6cz4 coloured by chain, front view.
PDB entry 6cz4 coloured by chain, side view.
PDB entry 6cz4 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Small molecule inhibitors reveal PTK6 kinase is not an oncogenic driver in breast cancers.
Qiu L, Levine K, Gajiwala KS, Cronin CN, Nagata A, Johnson E, Kraus M, Tatlock J, Kania R, Foley T, Sun S
PLoS One 13 e0198374 (2018)
PMID: 29879184

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-171829 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Protein-tyrosine kinase 6 Chain: A
Molecule details ›
Chain: A
Length: 264 amino acids
Theoretical weight: 30.25 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: Q13882 (Residues: 182-443; Coverage: 58%)
Gene names: BRK, PTK6
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand FKY 1 x FKY
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 17-ID
Spacegroup: P212121
Unit cell:
a: 37.914Å b: 54.873Å c: 134.629Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.203 0.203 0.209
Expression system: Spodoptera frugiperda

Quick links

Citations

4 review citations

Putting the BRK on breast cancer: From molecular target to therapeutics.
Ang et al. (2021)
3 more

2 mentions without citation

Small molecule inhibitors reveal PTK6 kinase is not an oncogenic driver in breast cancers.
Qiu et al. (2018)
1 more