› 3ua8

X-ray diffraction
1.9Å resolution

Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2

Released:
DOI: 10.2210/pdb3ua8/pdb
PDB entry 3ua8 coloured by chain, front view.
PDB entry 3ua8 coloured by chain, side view.
PDB entry 3ua8 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.
Orain D, Ofner S, Koller M, Carcache DA, Froestl W, Allgeier H, Rasetti V, Nozulak J, Mattes H, Soldermann N, Floersheim P, Desrayaud S, Kallen J, Lingenhoehl K, Urwyler S
Bioorg Med Chem Lett 22 996-9 (2012)
PMID: 22197388

Function and Biology Details

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

Structure analysis Details

Assembly composition:
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-154589 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Glutamate receptor 2 Chain: A
Molecule details ›
Chain: A
Length: 263 amino acids
Theoretical weight: 29.35 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P42262 (Residues: 413-527, 653-796; Coverage: 30%)
Gene names: GLUR2, GRIA2, GluA2
Sequence domains:
Structure domains: Periplasmic binding protein-like II

Ligands and Environments

1 bound ligand:
Ligand 08W 1 x 08W
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SLS BEAMLINE X10SA
Spacegroup: P21212
Unit cell:
a: 51.181Å b: 104.548Å c: 49.441Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.185 0.184 0.215
Expression system: Escherichia coli

Quick links

Citations

4 review citations

AMPA receptors as a molecular target in epilepsy therapy.
Rogawski MA. (2013)
3 more

3 mentions without citation

Structure and organization of heteromeric AMPA-type glutamate receptors.
Herguedas et al. (2016)
2 more