› 6byz

X-ray diffraction
2.96Å resolution

Structure of Cysteine-free Human Insulin-Degrading Enzyme in complex with Substrate-selective Macrocyclic Inhibitor 37

Released:
DOI: 10.2210/pdb6byz/pdb
PDB entry 6byz coloured by chain, front view.
PDB entry 6byz coloured by chain, side view.
PDB entry 6byz coloured by chain, top view.
Source organisms:
Primary publication:
Substrate-selective inhibitors that reprogram the activity of insulin-degrading enzyme.
Maianti JP, Tan GA, Vetere A, Welsh AJ, Wagner BK, Seeliger MA, Liu DR
Nat Chem Biol 15 565-574 (2019)
PMID: 31086331

Function and Biology Details

Reaction catalysed: 
Degradation of insulin, glucagon and other polypeptides. No action on proteins.
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
hetero dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-147043 (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Insulin-degrading enzyme Chains: A, B
Molecule details ›
Chains: A, B
Length: 1019 amino acids
Theoretical weight: 117.97 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P14735 (Residues: 1-1019; Coverage: 100%)
Gene name: IDE
Sequence domains:
Structure domains: Metalloenzyme, LuxS/M16 peptidase-like
ALA-ALA-ALA Chains: D, E
Molecule details ›
Chains: D, E
Length: 3 amino acids
Theoretical weight: 231 Da
Source organism: Escherichia coli BL21(DE3)

Ligands and Environments

2 bound ligands:
Ligand J18 2 x J18
Ligand EPE 2 x EPE
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 12.3.1
Spacegroup: P65
Unit cell:
a: 264.486Å b: 264.486Å c: 91.094Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.162 0.161 0.203
Expression system: Escherichia coli BL21(DE3)

Quick links

Citations

9 review citations

Targeting Insulin-Degrading Enzyme in Insulin Clearance.
Leissring et al. (2021)
8 more

1 mention without citation

Substrate-selective inhibitors that reprogram the activity of insulin-degrading enzyme.
Maianti et al. (2019)