› 7lci

Electron Microscopy
2.9Å resolution

PF 06882961 bound to the glucagon-like peptide-1 receptor (GLP-1R):Gs complex

Released:
DOI: 10.2210/pdb7lci/pdb
PDB entry 7lci coloured by chain, front view.
PDB entry 7lci coloured by chain, side view.
PDB entry 7lci coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Evolving cryo-EM structural approaches for GPCR drug discovery.
Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ
Structure 29 963-974.e6 (2021)
PMID: 33957078
Related structures: EMD-23274

Function and Biology Details

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

Structure analysis Details

Assembly composition:
hetero tetramer (preferred)
PDBe Complex ID:
PDB-CPX-154980 (preferred)
Entry contents:
4 distinct polypeptide molecules
Macromolecules (4 distinct):
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:
Guanine nucleotide-binding protein G(s) subunit alpha isoforms short Chain: A
Molecule details ›
Chain: A
Length: 394 amino acids
Theoretical weight: 45.7 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

Ligands and Environments

1 bound ligand:
Ligand UK4 1 x UK4
No modified residues

Experiments and Validation Details

Entry percentile scores
Resolution: 2.9Å
Relevant EMDB volumes: EMD-23274
Expression system: Trichoplusia ni

Quick links

Citations

4 review citations

Targeting VIP and PACAP Receptor Signaling: New Insights into Designing Drugs for the PACAP Subfamily of Receptors.
Lu et al. (2022)
3 more

8 mentions without citation

Evolving Experimental Techniques for Structure-Based Drug Design.
Aplin et al. (2022)
7 more