› 5ee7

X-ray diffraction
2.5Å resolution

Crystal structure of the human glucagon receptor (GCGR) in complex with the antagonist MK-0893

Released:
DOI: 10.2210/pdb5ee7/pdb
PDB entry 5ee7 coloured by chain, front view.
PDB entry 5ee7 coloured by chain, side view.
PDB entry 5ee7 coloured by chain, top view.
Source organisms:
Primary publication:
Extra-helical binding site of a glucagon receptor antagonist.
Jazayeri A, Doré AS, Lamb D, Krishnamurthy H, Southall SM, Baig AH, Bortolato A, Koglin M, Robertson NJ, Errey JC, Andrews SP, Teobald I, Brown AJ, Cooke RM, Weir M, Marshall FH
Nature 533 274-7 (2016)
PMID: 27111510

Function and Biology Details

Reaction catalysed: 
Hydrolysis of (1->4)-beta-linkages between N-acetylmuramic acid and N-acetyl-D-glucosamine residues in a peptidoglycan and between N-acetyl-D-glucosamine residues in chitodextrins
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-132992 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Endolysin; Glucagon receptor Chain: A
Molecule details ›
Chain: A
Length: 452 amino acids
Theoretical weight: 51.28 KDa
Source organisms: Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P47871 (Residues: 136-254, 259-417; Coverage: 62%)
  • Canonical: P00720 (Residues: 2-160; Coverage: 97%)
Gene names: E, GCGR
Sequence domains:

Ligands and Environments

4 bound ligands:
Ligand 5MV 1 x 5MV
Ligand OLA 14 x OLA
Ligand PE5 1 x PE5
Ligand TLA 1 x TLA
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: DIAMOND BEAMLINE I04
Spacegroup: P212121
Unit cell:
a: 37.583Å b: 71.476Å c: 183.108Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.228 0.226 0.262
Expression system: Spodoptera frugiperda

Quick links

Citations

24 review citations

Biased signalling: from simple switches to allosteric microprocessors.
Smith et al. (2018)
23 more

48 mentions without citation

Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes.
Graaf et al. (2016)
47 more