› 6d9h

Electron Microscopy
3.6Å resolution

Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist

Released:
DOI: 10.2210/pdb6d9h/pdb
PDB entry 6d9h coloured by chain, front view.
PDB entry 6d9h coloured by chain, side view.
PDB entry 6d9h coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structure of the adenosine-bound human adenosine A1 receptor-Gi complex.
Draper-Joyce CJ, Khoshouei M, Thal DM, Liang YL, Nguyen ATN, Furness SGB, Venugopal H, Baltos JA, Plitzko JM, Danev R, Baumeister W, May LT, Wootten D, Sexton PM, Glukhova A, Christopoulos A
Nature 558 559-563 (2018)
PMID: 29925945
Related structures: EMD-7835

Function and Biology Details

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

Structure analysis Details

Assembly composition:
hetero tetramer (preferred)
PDBe Complex ID:
PDB-CPX-138246 (preferred)
Entry contents:
4 distinct polypeptide molecules
Macromolecules (4 distinct):
Guanine nucleotide-binding protein G(i) subunit alpha-2 Chain: A
Molecule details ›
Chain: A
Length: 355 amino acids
Theoretical weight: 40.5 KDa
Source organism: Homo sapiens
Expression system: Trichoplusia ni
UniProt:
  • Canonical: P04899 (Residues: 1-355; Coverage: 100%)
Gene names: GNAI2, GNAI2B
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: 350 amino acids
Theoretical weight: 38.53 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
Structure domains: YVTN repeat-like/Quinoprotein amine dehydrogenase
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
Structure domains: Transducin (heterotrimeric G protein), gamma chain
Adenosine receptor A1; Muscarinic acetylcholine receptor M4 Chain: R
Molecule details ›
Chain: R
Length: 389 amino acids
Theoretical weight: 43.54 KDa
Source organism: Homo sapiens
Expression system: Trichoplusia ni
UniProt:
  • Canonical: P08173 (Residues: 2-23; Coverage: 5%)
  • Canonical: P30542 (Residues: 2-326; Coverage: 100%)
Gene names: ADORA1, CHRM4
Sequence domains: 7 transmembrane receptor (rhodopsin family)
Structure domains: Rhodopsin 7-helix transmembrane proteins

Ligands and Environments

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

Experiments and Validation Details

Entry percentile scores
Resolution: 3.6Å
Relevant EMDB volumes: EMD-7835
Expression system: Trichoplusia ni

Quick links

Citations

27 review citations

Adenosine A2A receptor antagonists: from caffeine to selective non-xanthines.
Jacobson et al. (2022)
26 more

57 mentions without citation

G protein-coupled receptors: structure- and function-based drug discovery.
Yang et al. (2021)
56 more