› 5y5u

X-ray diffraction
2.14Å resolution

Crystal structures of spleen tyrosine kinase in complex with a novel inhibitor

Released:
DOI: 10.2210/pdb5y5u/pdb
PDB entry 5y5u coloured by chain, front view.
PDB entry 5y5u coloured by chain, side view.
PDB entry 5y5u coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Crystal Structures of Spleen Tyrosine Kinase in Complex with Two Novel 4-Aminopyrido[4,3-d] Pyrimidine Derivative Inhibitors.
Lee SJ, Choi JS, Bong SM, Hwang HJ, Lee J, Song HJ, Lee J, Kim JH, Koh JS, Lee BI
Mol Cells 41 545-552 (2018)
PMID: 29890824

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: 293 amino acids
Theoretical weight: 34.22 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 8OU 2 x 8OU
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SPRING-8 BEAMLINE BL26B1
Spacegroup: P1
Unit cell:
a: 40.155Å b: 42.013Å c: 87.66Å
α: 79.83° β: 90.78° γ: 79.6°
R-values:
R R work R free
0.239 0.238 0.26
Expression system: Spodoptera frugiperda

Quick links

Citations

4 mentions without citation

Synthesis, In Vitro and In Silico Anticancer Activity of New 4-Methylbenzamide Derivatives Containing 2,6-Substituted Purines as Potential Protein Kinases Inhibitors.
Kalinichenko et al. (2021)
3 more