› 5zg3

X-ray diffraction
1.65Å resolution

Crystal structure of the GluA2o LBD in complex with glutamate and TAK-137

Released:
DOI: 10.2210/pdb5zg3/pdb
PDB entry 5zg3 coloured by chain, front view.
PDB entry 5zg3 coloured by chain, side view.
PDB entry 5zg3 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window.
Kunugi A, Tanaka M, Suzuki A, Tajima Y, Suzuki N, Suzuki M, Nakamura S, Kuno H, Yokota A, Sogabe S, Kosugi Y, Awasaki Y, Kaku T, Kimura H
Neuropsychopharmacology 44 961-970 (2019)
PMID: 30209408

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 Chains: A, B, C, D, E, F
Molecule details ›
Chains: A, B, C, D, E, F
Length: 263 amino acids
Theoretical weight: 29.34 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

4 bound ligands:
Ligand 9C6 3 x 9C6
Ligand GLU 6 x GLU
Ligand ZN 12 x ZN
Ligand ACT 11 x ACT
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.3
Spacegroup: P21
Unit cell:
a: 114.065Å b: 162.332Å c: 47.385Å
α: 90° β: 90.02° γ: 90°
R-values:
R R work R free
0.186 0.184 0.215
Expression system: Escherichia coli

Quick links

Citations

2 review citations

Cryo-EM as a powerful tool for drug discovery.
Van Drie et al. (2020)
1 more

1 mention without citation

Screening for Neuroprotective and Rapid Antidepressant-like Effects of 20 Essential Oils.
Tran et al. (2023)