› 8ef5

Electron Microscopy
3.3Å resolution

Fentanyl-bound mu-opioid receptor-Gi complex

Released:
DOI: 10.2210/pdb8ef5/pdb
PDB entry 8ef5 coloured by chain, front view.
PDB entry 8ef5 coloured by chain, side view.
PDB entry 8ef5 coloured by chain, top view.
Source organisms:
Primary publication:
Molecular recognition of morphine and fentanyl by the human μ-opioid receptor.
Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE
Cell 185 4361-4375.e19 (2022)
PMID: 36368306
Related structures: EMD-28066

Function and Biology Details

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

Structure analysis Details

Assembly composition:
hetero heptamer (preferred)
PDBe Complex ID:
PDB-CPX-273605 (preferred)
Entry contents:
5 distinct polypeptide molecules
Macromolecules (5 distinct):
Mu-type opioid receptor Chains: M, R
Molecule details ›
Chains: M, R
Length: 367 amino acids
Theoretical weight: 41.07 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P35372 (Residues: 2-368; Coverage: 92%)
Gene names: MOR1, OPRM1
Sequence domains: 7 transmembrane receptor (rhodopsin family)
Guanine nucleotide-binding protein G(i) subunit alpha-1 Chains: A, F
Molecule details ›
Chains: A, F
Length: 354 amino acids
Theoretical weight: 40.45 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: 353 amino acids
Theoretical weight: 39.02 KDa
Source organism: Rattus norvegicus
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P54311 (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: Bos taurus
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P63212 (Residues: 1-68; Coverage: 96%)
Gene name: GNG2
Sequence domains: GGL domain
scFv16 Chain: E
Molecule details ›
Chain: E
Length: 248 amino acids
Theoretical weight: 26.41 KDa
Source organism: synthetic construct
Expression system: Escherichia coli

Ligands and Environments

2 bound ligands:
Ligand 7V7 2 x 7V7
Ligand CLR 10 x CLR
No modified residues

Experiments and Validation Details

Entry percentile scores
Resolution: 3.3Å
Relevant EMDB volumes: EMD-28066
Expression systems:
  • Spodoptera frugiperda
  • Escherichia coli

Quick links

Citations

7 review citations

Opioids and opioid receptors; understanding pharmacological mechanisms as a key to therapeutic advances and mitigation of the misuse crisis.
Lambert DG. (2023)
6 more

10 mentions without citation

IUPHAR themed review: Opioid efficacy, bias, and selectivity.
Ramos-Gonzalez et al. (2023)
9 more