› 6orv

Electron Microscopy
3Å resolution

Non-peptide agonist (TT-OAD2) bound to the Glucagon-Like peptide-1 (GLP-1) Receptor

Released:
DOI: 10.2210/pdb6orv/pdb
PDB entry 6orv coloured by chain, front view.
PDB entry 6orv coloured by chain, side view.
PDB entry 6orv coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Activation of the GLP-1 receptor by a non-peptidic agonist.
Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, Miller LJ, Reynolds CA, Danev R, Sexton PM, Wootten D
Nature 577 432-436 (2020)
PMID: 31915381
Related structures: EMD-20179

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-211232 (preferred)
Entry contents:
5 distinct polypeptide molecules
Macromolecules (5 distinct):
Guanine nucleotide-binding protein G(s) subunit alpha isoforms short Chain: AP
Molecule details ›
Chain: AP
Length: 394 amino acids
Theoretical weight: 45.68 KDa
Source organism: Homo sapiens
Expression system: Trichoplusia ni
UniProt:
  • Canonical: P63092 (Residues: 1-394; Coverage: 100%)
Gene names: GNAS, GNAS1, GSP
Sequence domains: G-protein alpha subunit
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 Chain: BP
Molecule details ›
Chain: BP
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
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 Chain: GP
Molecule details ›
Chain: GP
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
Nanobody 35 Chain: NP
Molecule details ›
Chain: NP
Length: 138 amino acids
Theoretical weight: 15.14 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
Glucagon-like peptide 1 receptor Chain: RP
Molecule details ›
Chain: RP
Length: 491 amino acids
Theoretical weight: 56.75 KDa
Source organism: Homo sapiens
Expression system: Trichoplusia ni
UniProt:
  • Canonical: P43220 (Residues: 24-463; Coverage: 100%)
Gene name: GLP1R
Sequence domains:

Ligands and Environments

1 bound ligand:
Ligand N2V 1 x N2V
No modified residues

Experiments and Validation Details

Entry percentile scores
Resolution: 3Å
Relevant EMDB volumes: EMD-20179
Expression systems:
  • Trichoplusia ni
  • Escherichia coli

Quick links

Citations

14 review citations

Glucagon-like peptide-1 (GLP-1)-based receptor agonists as a treatment for Parkinson's disease.
Glotfelty et al. (2020)
13 more

10 mentions without citation

Non-peptide agonists and positive allosteric modulators of glucagon-like peptide-1 receptors: Alternative approaches for treatment of Type 2 diabetes.
Malik et al. (2022)
9 more