› 4lz7

X-ray diffraction
2.1Å resolution

Crystal structures of GLuR2 ligand-binding-domain in complex with glutamate and positive allosteric modulators

Released:
DOI: 10.2210/pdb4lz7/pdb
PDB entry 4lz7 coloured by chain, front view.
PDB entry 4lz7 coloured by chain, side view.
PDB entry 4lz7 coloured by chain, top view.
Source organism: Rattus norvegicus
Primary publication:
Discovery and characterization of a novel dihydroisoxazole class of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiators.
Patel NC, Schwarz J, Hou XJ, Hoover DJ, Xie L, Fliri AJ, Gallaschun RJ, Lazzaro JT, Bryce DK, Hoffmann WE, Hanks AN, McGinnis D, Marr ES, Gazard JL, Hajós M, Scialis RJ, Hurst RS, Shaffer CL, Pandit J, O'Donnell CJ
J Med Chem 56 9180-91 (2013)
PMID: 24215237

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-148607 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Glutamate receptor 2 Chains: A, B, C
Molecule details ›
Chains: A, B, C
Length: 275 amino acids
Theoretical weight: 30.34 KDa
Source organism: Rattus norvegicus
Expression system: Escherichia coli
UniProt:
  • Canonical: P19491 (Residues: 404-527, 653-796; Coverage: 31%)
Gene names: GluA2, Glur2, Gria2
Sequence domains:
Structure domains: Periplasmic binding protein-like II

Ligands and Environments

3 bound ligands:
Ligand ZN 5 x ZN
Ligand GLU 3 x GLU
Ligand 1YW 2 x 1YW
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU MICROMAX-007 HF
Spacegroup: P21212
Unit cell:
a: 114.38Å b: 164.344Å c: 47.402Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.198 0.196 0.24
Expression system: Escherichia coli

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Citations

3 review citations

AMPA receptor-positive allosteric modulators for the treatment of schizophrenia: an overview of recent patent applications.
Ward et al. (2015)
2 more