› 6pt0

Electron Microscopy
3.2Å resolution

Cryo-EM structure of human cannabinoid receptor 2-Gi protein in complex with agonist WIN 55,212-2

Released:
DOI: 10.2210/pdb6pt0/pdb
PDB entry 6pt0 coloured by chain, front view.
PDB entry 6pt0 coloured by chain, side view.
PDB entry 6pt0 coloured by chain, top view.
Source organisms:
Primary publication:
Cryo-EM Structure of the Human Cannabinoid Receptor CB2-Gi Signaling Complex.
Xing C, Zhuang Y, Xu TH, Feng Z, Zhou XE, Chen M, Wang L, Meng X, Xue Y, Wang J, Liu H, McGuire TF, Zhao G, Melcher K, Zhang C, Xu HE, Xie XQ
Cell 180 645-654.e13 (2020)
PMID: 32004460
Related structures: EMD-20470

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-211083 (preferred)
Entry contents:
5 distinct polypeptide molecules
Macromolecules (5 distinct):
Cannabinoid receptor 2 Chain: R
Molecule details ›
Chain: R
Length: 369 amino acids
Theoretical weight: 40.76 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P34972 (Residues: 1-360; Coverage: 100%)
Gene names: CB2A, CB2B, CNR2
Sequence domains: 7 transmembrane receptor (rhodopsin family)
Guanine nucleotide-binding protein G(i) subunit alpha-1 Chain: A
Molecule details ›
Chain: A
Length: 354 amino acids
Theoretical weight: 40.41 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P63096 (Residues: 1-354; Coverage: 100%)
Gene name: GNAI1
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: 354 amino acids
Theoretical weight: 39.15 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
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: C
Molecule details ›
Chain: C
Length: 68 amino acids
Theoretical weight: 7.56 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P59768 (Residues: 1-68; Coverage: 96%)
Gene name: GNG2
Sequence domains: GGL domain
scFv16 Chain: E
Molecule details ›
Chain: E
Length: 259 amino acids
Theoretical weight: 27.78 KDa
Source organism: synthetic construct
Expression system: Escherichia coli

Ligands and Environments

3 bound ligands:
Ligand WI5 1 x WI5
Ligand PLM 4 x PLM
Ligand CLR 4 x CLR
No modified residues

Experiments and Validation Details

Entry percentile scores
Resolution: 3.2Å
Relevant EMDB volumes: EMD-20470
Expression systems:
  • Spodoptera frugiperda
  • Escherichia coli

Quick links

Citations

16 review citations

Covalent allosteric modulation: An emerging strategy for GPCRs drug discovery.
Bian et al. (2020)
15 more

44 mentions without citation

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