› 3fqh

X-ray diffraction
2.26Å resolution

Crystal structure of spleen tyrosine kinase complexed with a 2-substituted 7-azaindole

Released:
DOI: 10.2210/pdb3fqh/pdb
PDB entry 3fqh coloured by chain, front view.
PDB entry 3fqh coloured by chain, side view.
PDB entry 3fqh coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structural insights for design of potent spleen tyrosine kinase inhibitors from crystallographic analysis of three inhibitor complexes.
Villaseñor AG, Kondru R, Ho H, Wang S, Papp E, Shaw D, Barnett JW, Browner MF, Kuglstatter A
Chem Biol Drug Des 73 466-70 (2009)
PMID: 19220318

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 Chains: A, B
Molecule details ›
Chains: A, B
Length: 291 amino acids
Theoretical weight: 33.88 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P43405 (Residues: 356-635; Coverage: 44%)
Gene name: SYK
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand 057 2 x 057
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.1
Spacegroup: P1
Unit cell:
a: 40.156Å b: 41.949Å c: 87.604Å
α: 80.78° β: 90.78° γ: 79.59°
R-values:
R R work R free
0.216 0.214 0.259
Expression system: Spodoptera frugiperda

Quick links

Citations

8 review citations

The Src, Syk, and Tec family kinases: distinct types of molecular switches.
Bradshaw JM. (2010)
7 more

2 mentions without citation

The azaindole framework in the design of kinase inhibitors.
Mérour et al. (2014)
1 more