› 6ruq

X-ray diffraction
4.65Å resolution

Structure of GluA2cryst in complex the antagonist ZK200775 and the negative allosteric modulator GYKI53655 at 4.65 A resolution

Released:
DOI: 10.2210/pdb6ruq/pdb
Model geometry
Fit model/data
PDB entry 6ruq coloured by chain, front view.
PDB entry 6ruq coloured by chain, side view.
PDB entry 6ruq coloured by chain, top view.
Source organism: Rattus norvegicus
Primary publication:
Binding of a negative allosteric modulator and competitive antagonist can occur simultaneously at the ionotropic glutamate receptor GluA2.
Krintel C, Dorosz J, Larsen AH, Thorsen TS, Venskutonytė R, Mirza O, Gajhede M, Boesen T, Kastrup JS
FEBS J 288 995-1007 (2021)
PMID: 32543078

Function and Biology Details

Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
homo tetramer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-148611 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecules (3 distinct):
Glutamate receptor 2 Chains: A, B, C, D
Molecule details ›
Chains: A, B, C, D
Length: 823 amino acids
Theoretical weight: 92.03 KDa
Source organism: Rattus norvegicus
Expression system: Spodoptera
UniProt:
  • Canonical: P19491 (Residues: 25-847; Coverage: 95%)
Gene names: GluA2, Glur2, Gria2
Sequence domains:

Ligands and Environments

Carbohydrate polymer : NEW Components: NAG, BMA
Carbohydrate polymer
Carbohydrate polymer : NEW Components: NAG, BMA
Carbohydrate polymer
2 bound ligands:
Ligand GYK 4 x GYK
Ligand ZK1 4 x ZK1
No modified residues

Experiments and Validation Details

wwPDB Validation report is not available for this entry.
X-ray source: ESRF BEAMLINE ID29
Spacegroup: P21
Unit cell:
a: 91.773Å b: 306.596Å c: 107.728Å
α: 90° β: 94.264° γ: 90°
R-values:
R R work R free
0.245 0.242 0.291
Expression system: Spodoptera

Quick links

Citations

1 review citation

Diversity of AMPA Receptor Ligands: Chemotypes, Binding Modes, Mechanisms of Action, and Therapeutic Effects.
Golubeva et al. (2022)
5 other articles

1 mention without citation

Evolution of glutamatergic signaling and synapses.
Moroz et al. (2021)

PDB-REDO

The sliders below show the change in model quality between original PDB entry and the PDB-REDO entry

Model Geometry
 
 
Data not available
DNA/RNA Geometry
 
 
Data not available
Fit model/data
 
 
Data not available
PDB-REDO