› 6hup

Electron Microscopy
3.58Å resolution

CryoEM structure of human full-length alpha1beta3gamma2L GABA(A)R in complex with diazepam (Valium), GABA and megabody Mb38.

Released:
DOI: 10.2210/pdb6hup/pdb
PDB entry 6hup coloured by chain, front view.
PDB entry 6hup coloured by chain, side view.
PDB entry 6hup coloured by chain, top view.
Source organisms:
Primary publication:
GABAA receptor signalling mechanisms revealed by structural pharmacology.
Masiulis S, Desai R, Uchański T, Serna Martin I, Laverty D, Karia D, Malinauskas T, Zivanov J, Pardon E, Kotecha A, Steyaert J, Miller KW, Aricescu AR
OpenAccess logo Nature 565 454-459 (2019)
PMID: 30602790
Related structures: EMD-0283

Function and Biology Details

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

Structure analysis Details

Assembly composition:
hetero hexamer (preferred)
PDBe Complex ID:
PDB-CPX-290950 (preferred)
Entry contents:
4 distinct polypeptide molecules
Macromolecules (8 distinct):
Gamma-aminobutyric acid receptor subunit alpha-1 Chains: A, D
Molecule details ›
Chains: A, D
Length: 464 amino acids
Theoretical weight: 52.92 KDa
Source organisms: Expression system: Homo sapiens
UniProt:
  • Canonical: P14867 (Residues: 1-1, 28-456; Coverage: 94%)
  • Canonical: P08219 (Residues: 2-27; Coverage: 0%)
Gene name: GABRA1
Sequence domains:
Gamma-aminobutyric acid receptor subunit beta-3 Chains: B, E
Molecule details ›
Chains: B, E
Length: 473 amino acids
Theoretical weight: 54.44 KDa
Source organism: Homo sapiens
Expression system: Homo sapiens
UniProt:
  • Canonical: P28472 (Residues: 26-473; Coverage: 100%)
  • Best match: P28472-2 (Residues: 1-473)
Gene name: GABRB3
Sequence domains:
Gamma-aminobutyric acid receptor subunit gamma-2 Chain: C
Megabody Mb38 Chain: G

Ligands and Environments

Carbohydrate polymer : NEW Components: NAG, BMA, MAN
Carbohydrate polymer
Carbohydrate polymer : NEW Components: NAG
Carbohydrate polymer
Carbohydrate polymer : NEW Components: NAG, BMA, MAN
Carbohydrate polymer
Carbohydrate polymer : NEW Components: NAG, BMA, MAN
Carbohydrate polymer
3 bound ligands:
Ligand PIO 2 x PIO
Ligand ABU 2 x ABU
Ligand DZP 3 x DZP
No modified residues

Experiments and Validation Details

wwPDB Validation report is not available for this EM entry.
Resolution: 3.58Å
Relevant EMDB volumes: EMD-0283
Expression systems:
  • Homo sapiens
  • Escherichia coli

Quick links

Citations

45 review citations

A guide to: generation and design of nanobodies.
Muyldermans S. (2021)
44 more

35 mentions without citation

Direct Structural Insights into GABAA Receptor Pharmacology.
Kim et al. (2021)
34 more