› 3srv

X-ray diffraction
1.95Å resolution

Crystal structure of spleen tyrosine kinase (SYK) in complex with a diaminopyrimidine carboxamide inhibitor

Released:
DOI: 10.2210/pdb3srv/pdb
PDB entry 3srv coloured by chain, front view.
PDB entry 3srv coloured by chain, side view.
PDB entry 3srv coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
Liddle J, Atkinson FL, Barker MD, Carter PS, Curtis NR, Davis RP, Douault C, Dickson MC, Elwes D, Garton NS, Gray M, Hayhow TG, Hobbs CI, Jones E, Leach S, Leavens K, Lewis HD, McCleary S, Neu M, Patel VK, Preston AG, Ramirez-Molina C, Shipley TJ, Skone PA, Smithers N, Somers DO, Walker AL, Watson RJ, Weingarten GG
Bioorg Med Chem Lett 21 6188-94 (2011)
PMID: 21903390

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:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Tyrosine-protein kinase SYK Chain: A
Molecule details ›
Chain: A
Length: 277 amino acids
Theoretical weight: 32.16 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P43405 (Residues: 360-635; Coverage: 44%)
Gene name: SYK
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:
Tyrosine-protein kinase SYK Chain: B
Molecule details ›
Chain: B
Length: 277 amino acids
Theoretical weight: 32.08 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P43405 (Residues: 360-635; Coverage: 44%)
Gene name: SYK
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand S19 2 x S19
Ligand GOL 4 x GOL
1 modified residue:
Ligand PTR 1 x PTR

Experiments and Validation Details

Entry percentile scores
X-ray source: ESRF BEAMLINE ID29
Spacegroup: P1
Unit cell:
a: 40.124Å b: 42.316Å c: 87.621Å
α: 99.68° β: 90.16° γ: 100.19°
R-values:
R R work R free
0.188 0.185 0.241
Expression system: Spodoptera frugiperda

Quick links

Citations

6 review citations

Getting Syk: spleen tyrosine kinase as a therapeutic target.
Geahlen RL. (2014)
5 more

2 mentions without citation

Exploration of the mechanism by which Huangqi Guizhi Wuwu decoction inhibits Lps-induced inflammation by regulating macrophage polarization based on network pharmacology.
Wang et al. (2023)
1 more