› 4rx7

X-ray diffraction
1.8Å resolution

SYK Catalytic Domain Complexed with a Potent Triazine Inhibitor

Released:
DOI: 10.2210/pdb4rx7/pdb
PDB entry 4rx7 coloured by chain, front view.
PDB entry 4rx7 coloured by chain, side view.
PDB entry 4rx7 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Discovery and profiling of a selective and efficacious Syk inhibitor.
Thoma G, Smith AB, van Eis MJ, Vangrevelinghe E, Blanz J, Aichholz R, Littlewood-Evans A, Lee CC, Liu H, Zerwes HG
J Med Chem 58 1950-63 (2015)
PMID: 25633741

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: 289 amino acids
Theoretical weight: 33.67 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

3 bound ligands:
Ligand FMT 1 x FMT
Ligand GOL 1 x GOL
Ligand 3YV 1 x 3YV
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.3
Spacegroup: P212121
Unit cell:
a: 39.85Å b: 85.23Å c: 89.61Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.182 0.181 0.203
Expression system: Spodoptera frugiperda

Quick links

Citations

8 citation in other articles

The Novel Oral Syk Inhibitor, Bl1002494, Protects Mice From Arterial Thrombosis and Thromboinflammatory Brain Infarction.
van Eeuwijk et al. (2016)
7 more