› 6x1a

Electron Microscopy
2.5Å resolution

Non peptide agonist PF-06882961, bound to Glucagon-Like peptide-1 (GLP-1) Receptor

Released:
DOI: 10.2210/pdb6x1a/pdb
PDB entry 6x1a coloured by chain, front view.
PDB entry 6x1a coloured by chain, side view.
PDB entry 6x1a coloured by chain, top view.
Source organisms:
Primary publication:
Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists.
Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, ล enel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D
Mol Cell 80 485-500.e7 (2020)
PMID: 33027691
Related structures: EMD-21994

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-211234 (preferred)
Entry contents:
5 distinct polypeptide molecules
Macromolecules (5 distinct):
Guanine nucleotide-binding protein G(s) subunit alpha isoforms short Chain: A
Molecule details ›
Chain: A
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: B
Molecule details ›
Chain: B
Length: 340 amino acids
Theoretical weight: 37.41 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: G
Molecule details ›
Chain: G
Length: 58 amino acids
Theoretical weight: 6.38 KDa
Source organism: Homo sapiens
Expression system: Trichoplusia ni
UniProt:
  • Canonical: P59768 (Residues: 5-62; Coverage: 82%)
Gene name: GNG2
Sequence domains: GGL domain
Nanobody35 Chain: N
Molecule details ›
Chain: N
Length: 128 amino acids
Theoretical weight: 13.89 KDa
Source organism: Lama glama
Expression system: Escherichia coli
Glucagon-like peptide 1 receptor Chain: R
Molecule details ›
Chain: R
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 UK4 1 x UK4
No modified residues

Experiments and Validation Details

Entry percentile scores
Resolution: 2.5Å
Relevant EMDB volumes: EMD-21994
Expression systems:
  • Trichoplusia ni
  • Escherichia coli

Quick links

Citations

6 review citations

The therapeutic potential of GLP-1 receptor biased agonism.
Jones B. (2022)
5 more

15 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)
14 more