› 8jr9

Electron Microscopy
2.57Å resolution

Small molecule agonist (PCO371) bound to human parathyroid hormone receptor type 1 (PTH1R)

Released:
DOI: 10.2210/pdb8jr9/pdb
PDB entry 8jr9 coloured by chain, front view.
PDB entry 8jr9 coloured by chain, side view.
PDB entry 8jr9 coloured by chain, top view.
Source organisms:
Primary publication:
Conserved class B GPCR activation by a biased intracellular agonist.
Zhao LH, He Q, Yuan Q, Gu Y, He X, Shan H, Li J, Wang K, Li Y, Hu W, Wu K, Shen J, Xu HE
Nature (2023)
PMID: 37524305
Related structures: EMD-36593

Function and Biology Details

Biochemical function:
Biological process:
Cellular component:

Structure analysis Details

Assembly composition:
hetero pentamer (preferred)
PDBe Complex ID:
PDB-CPX-273935 (preferred)
Entry contents:
5 distinct polypeptide molecules
Macromolecules (5 distinct):
Guanine nucleotide-binding protein G(i) subunit alpha-1; Guanine nucleotide-binding protein G(s) subunit alpha isoforms short Chain: A
Molecule details ›
Chain: A
Length: 361 amino acids
Theoretical weight: 41.88 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P63092 (Residues: 1-3, 27-67, 205-251, 266-394; Coverage: 56%)
  • Canonical: P63096 (Residues: 4-19, 61-181, 229-242; Coverage: 40%)
Gene names: GNAI1, GNAS, GNAS1, GSP
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: 352 amino acids
Theoretical weight: 38.33 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: G
Molecule details ›
Chain: G
Length: 71 amino acids
Theoretical weight: 7.86 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P59768 (Residues: 1-71; Coverage: 100%)
Gene name: GNG2
Sequence domains: GGL domain
Nanobody 35 Chain: N
Molecule details ›
Chain: N
Length: 140 amino acids
Theoretical weight: 15.34 KDa
Source organism: Mus musculus
Expression system: Escherichia coli
Parathyroid hormone/parathyroid hormone-related peptide receptor Chain: R
Molecule details ›
Chain: R
Length: 478 amino acids
Theoretical weight: 54.78 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: Q03431 (Residues: 27-502; Coverage: 84%)
Gene names: PTH1R, PTHR, PTHR1
Sequence domains:

Ligands and Environments

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

Experiments and Validation Details

Entry percentile scores
Resolution: 2.57Å
Relevant EMDB volumes: EMD-36593
Expression systems:
  • Spodoptera frugiperda
  • Escherichia coli

Quick links

Citations

5 review citations

G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery.
Zhang et al. (2024)
4 more

1 mention without citation

A promising small molecule binding pocket in class B GPCRs: expanding potential for drug development.
Xiao et al. (2023)