› 3tuc

X-ray diffraction
2.1Å resolution

Crystal structure of SYK kinase domain with 1-benzyl-N-(5-(6,7-dimethoxyquinolin-4-yloxy)pyridin-2-yl)-2-oxo-1,2-dihydropyridine-3-carboxamide

Released:
DOI: 10.2210/pdb3tuc/pdb
PDB entry 3tuc coloured by chain, front view.
PDB entry 3tuc coloured by chain, side view.
PDB entry 3tuc coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Identification of type-II inhibitors using kinase structures.
Lovering F, McDonald J, Whitlock GA, Glossop PA, Phillips C, Bent A, Sabnis Y, Ryan M, Fitz L, Lee J, Chang JS, Han S, Kurumbail R, Thorarensen A
Chem Biol Drug Des 80 657-64 (2012)
PMID: 22759374

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-155056 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Tyrosine-protein kinase SYK Chain: A
Molecule details ›
Chain: A
Length: 299 amino acids
Theoretical weight: 34.88 KDa
Source organism: Homo sapiens
Expression system: Not provided
UniProt:
  • Canonical: P43405 (Residues: 343-635; Coverage: 46%)
Gene name: SYK
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

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

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 17-ID
Spacegroup: P212121
Unit cell:
a: 48Å b: 69.47Å c: 83.61Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.216 0.213 0.285
Expression system: Not provided

Quick links

Citations

4 review citations

αC helix displacement as a general approach for allosteric modulation of protein kinases.
Palmieri et al. (2013)
3 more

2 mentions without citation

Spatial distribution of disease-associated variants in three-dimensional structures of protein complexes.
Gress et al. (2017)
1 more