› 4isu

X-ray diffraction
2.3Å resolution

Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with the antagonist (2R)-IKM-159 at 2.3A resolution.

Released:
DOI: 10.2210/pdb4isu/pdb
PDB entry 4isu coloured by chain, front view.
PDB entry 4isu coloured by chain, side view.
PDB entry 4isu coloured by chain, top view.
Source organism: Rattus norvegicus
Primary publication:
Studies on an (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor antagonist IKM-159: asymmetric synthesis, neuroactivity, and structural characterization.
Juknaitė L, Sugamata Y, Tokiwa K, Ishikawa Y, Takamizawa S, Eng A, Sakai R, Pickering DS, Frydenvang K, Swanson GT, Kastrup JS, Oikawa M
J Med Chem 56 2283-93 (2013)
PMID: 23432124

Function and Biology Details

Biochemical function:
Biological process:
  • not assigned
Cellular component:
Sequence domains:

Structure analysis Details

Assemblies composition:
homo dimer
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-148604 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Glutamate receptor 2 Chains: A, B, C, D
Molecule details ›
Chains: A, B, C, D
Length: 263 amino acids
Theoretical weight: 29.22 KDa
Source organism: Rattus norvegicus
Expression system: Escherichia coli
UniProt:
  • Canonical: P19491 (Residues: 413-527, 653-796; Coverage: 30%)
Gene names: GluA2, Glur2, Gria2
Sequence domains:
Structure domains: Periplasmic binding protein-like II

Ligands and Environments

3 bound ligands:
Ligand IKM 2 x IKM
Ligand SO4 6 x SO4
Ligand CL 8 x CL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: MAX II BEAMLINE I911-3
Spacegroup: P212121
Unit cell:
a: 62.514Å b: 88.773Å c: 194.456Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.189 0.185 0.258
Expression system: Escherichia coli

Quick links

Citations

2 review citations

Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels.
Hansen et al. (2021)
1 more

1 mention without citation

Studies on an (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor antagonist IKM-159: asymmetric synthesis, neuroactivity, and structural characterization.
Juknaitė et al. (2013)