› 8bhg

X-ray diffraction
2.39Å resolution

GABA-A receptor a5 heteromer - a5V2 - Bretazenil

Released:
DOI: 10.2210/pdb8bhg/pdb
PDB entry 8bhg coloured by chain, front view.
PDB entry 8bhg coloured by chain, side view.
PDB entry 8bhg coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
The molecular basis of drug selectivity for α5 subunit-containing GABAA receptors.
Kasaragod VB, Malinauskas T, Wahid AA, Lengyel J, Knoflach F, Hardwick SW, Jones CF, Chen WN, Lucas X, El Omari K, Chirgadze DY, Aricescu AR, Cecere G, Hernandez MC, Miller PS
OpenAccess logo Nat Struct Mol Biol (2023)
PMID: 37903907

Function and Biology Details

Biochemical function:
Biological process:
Cellular component:

Structure analysis Details

Assembly composition:
hetero pentamer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-235805 (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Gamma-aminobutyric acid receptor subunit alpha-5 Chains: A, C, D, E
Molecule details ›
Chains: A, C, D, E
Length: 350 amino acids
Theoretical weight: 40.15 KDa
Source organism: Homo sapiens
Expression system: Homo sapiens
UniProt:
  • Canonical: P31644 (Residues: 32-451; Coverage: 81%)
Gene name: GABRA5
Sequence domains:
Gamma-aminobutyric acid receptor subunit gamma-2 Chain: B
Molecule details ›
Chain: B
Length: 379 amino acids
Theoretical weight: 43.75 KDa
Source organism: Homo sapiens
Expression system: Homo sapiens
UniProt:
  • Canonical: P18507 (Residues: 40-359, 361-361, 362-378, 379-381, 382-391, 392-392, 393-396, 398-409; Coverage: 84%)
Gene name: GABRG2
Sequence domains:

Ligands and Environments

4 bound ligands:
Ligand QMU 5 x QMU
Ligand DMU 5 x DMU
Ligand NO3 3 x NO3
Ligand NAG 6 x NAG
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: DIAMOND BEAMLINE I04
Spacegroup: P21
Unit cell:
a: 81.14Å b: 137.637Å c: 113.351Å
α: 90° β: 106.06° γ: 90°
R-values:
R R work R free
0.259 0.257 0.284
Expression system: Homo sapiens

Quick links

Citations

1 mention without citation

The molecular basis of drug selectivity for α5 subunit-containing GABAA receptors.
Kasaragod et al. (2023)