› 5jwp

X-ray diffraction
2.1Å resolution

Crystal structure of human FIH D201E variant in complex with Zn, alpha-ketoglutarate, and HIF1 alpha peptide.

Released:
DOI: 10.2210/pdb5jwp/pdb
PDB entry 5jwp coloured by chain, front view.
PDB entry 5jwp coloured by chain, side view.
PDB entry 5jwp coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
The facial triad in the α-ketoglutarate dependent oxygenase FIH: A role for sterics in linking substrate binding to O2 activation.
Hangasky JA, Taabazuing CY, Martin CB, Eron SJ, Knapp MJ
J Inorg Biochem 166 26-33 (2017)
PMID: 27815979

Function and Biology Details

Reactions catalysed: 
Hypoxia-inducible factor-L-asparagine + 2-oxoglutarate + O(2) = hypoxia-inducible factor-(3S)-3-hydroxy-L-asparagine + succinate + CO(2)
[Ankyrin-repeat domain protein]-L-asparagine + 2-oxoglutarate + O(2) = [ankyrin-repeat domain protein]-(3S)-3-hydroxy-L-asparagine + succinate + CO(2)
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
hetero tetramer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-172550 (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Hypoxia-inducible factor 1-alpha inhibitor Chain: A
Molecule details ›
Chain: A
Length: 352 amino acids
Theoretical weight: 40.62 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: Q9NWT6 (Residues: 1-349; Coverage: 100%)
Gene names: FIH1, HIF1AN
Sequence domains: Cupin-like domain
Structure domains:
Hypoxia-inducible factor 1-alpha Chain: B
Molecule details ›
Chain: B
Length: 19 amino acids
Theoretical weight: 2.02 KDa
Source organism: Homo sapiens
Expression system: Not provided
UniProt:
  • Canonical: Q16665 (Residues: 788-806; Coverage: 2%)
Gene names: BHLHE78, HIF1A, MOP1, PASD8
Sequence domains: HIF-1 alpha C terminal transactivation domain

Ligands and Environments

4 bound ligands:
Ligand AKG 1 x AKG
Ligand GOL 1 x GOL
Ligand ZN 1 x ZN
Ligand SO4 4 x SO4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: NSLS BEAMLINE X6A
Spacegroup: P41212
Unit cell:
a: 86.22Å b: 86.22Å c: 149.903Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.173 0.17 0.209
Expression systems:
  • Escherichia coli BL21(DE3)
  • Not provided

Quick links

Citations

1 review citation

Bridging angiogenesis and immune evasion in the hypoxic tumor microenvironment.
Schito L. (2018)
6 other articles

6 mentions without citation

Hypoxia inducible factor (HIF) as a model for studying inhibition of protein-protein interactions.
Burslem et al. (2017)
5 more