› 7w7e

Electron Microscopy
3.4Å resolution

Cryo-EM structure of the alpha2A adrenergic receptor GoA signaling complex bound to a biased agonist

Released:
DOI: 10.2210/pdb7w7e/pdb
PDB entry 7w7e coloured by chain, front view.
PDB entry 7w7e coloured by chain, side view.
PDB entry 7w7e coloured by chain, top view.
Source organisms:
Primary publication:
Structure-based discovery of nonopioid analgesics acting through the α2A-adrenergic receptor.
Fink EA, Xu J, Hübner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P
Science 377 eabn7065 (2022)
PMID: 36173843
Related structures: EMD-32342

Function and Biology Details

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

Structure analysis Details

Assembly composition:
hetero pentamer (preferred)
PDBe Complex ID:
PDB-CPX-225115 (preferred)
Entry contents:
5 distinct polypeptide molecules
Macromolecules (5 distinct):
Guanine nucleotide-binding protein G(o) subunit alpha Chain: A
Molecule details ›
Chain: A
Length: 354 amino acids
Theoretical weight: 40.1 KDa
Source organism: Homo sapiens
Expression system: Trichoplusia ni
UniProt:
  • Canonical: P09471 (Residues: 1-354; Coverage: 100%)
Gene name: GNAO1
Sequence domains: G-protein alpha subunit
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 Chain: B
Molecule details ›
Chain: B
Length: 349 amino acids
Theoretical weight: 38.4 KDa
Source organism: Homo sapiens
Expression system: Trichoplusia ni
UniProt:
  • Canonical: P62873 (Residues: 2-340; Coverage: 100%)
Gene name: GNB1
Sequence domains: WD domain, G-beta repeat
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 Chain: G
Molecule details ›
Chain: G
Length: 71 amino acids
Theoretical weight: 7.86 KDa
Source organism: Homo sapiens
Expression system: Trichoplusia ni
UniProt:
  • Canonical: P59768 (Residues: 1-71; Coverage: 100%)
Gene name: GNG2
Sequence domains: GGL domain
scFv Chain: H
Molecule details ›
Chain: H
Length: 307 amino acids
Theoretical weight: 32.9 KDa
Source organism: Mus musculus
Expression system: Spodoptera frugiperda
Alpha-2A adrenergic receptor Chain: R
Molecule details ›
Chain: R
Length: 465 amino acids
Theoretical weight: 50.7 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P08913 (Residues: 1-465; Coverage: 100%)
Gene names: ADRA2A, ADRA2R, ADRAR
Sequence domains: 7 transmembrane receptor (rhodopsin family)

Ligands and Environments

1 bound ligand:
Ligand W58 1 x W58
No modified residues

Experiments and Validation Details

Entry percentile scores
Resolution: 3.4Å
Relevant EMDB volumes: EMD-32342
Expression systems:
  • Trichoplusia ni
  • Spodoptera frugiperda

Quick links

Citations

4 review citations

A Novel "Activation Switch" Motif Common to All Aminergic Receptors.
Lee et al. (2023)
3 more

2 mentions without citation

A Comprehensive Survey of Prospective Structure-Based Virtual Screening for Early Drug Discovery in the Past Fifteen Years.
Zhu et al. (2022)
1 more