› 3kcy

X-ray diffraction
2.59Å resolution

Factor inhibiting HIF-1 alpha in complex with 8-hydroxyquinoline

Released:
DOI: 10.2210/pdb3kcy/pdb
PDB entry 3kcy coloured by chain, front view.
PDB entry 3kcy coloured by chain, side view.
PDB entry 3kcy coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Crystal structures of human FIH-1 in complex with quinol family inhibitors.
Moon H, Han S, Park H, Choe J
Mol Cells 29 471-4 (2010)
PMID: 20396966

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:
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-192661 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Hypoxia-inducible factor 1-alpha inhibitor Chain: A
Molecule details ›
Chain: A
Length: 335 amino acids
Theoretical weight: 39.15 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: Q9NWT6 (Residues: 15-349; Coverage: 96%)
Gene names: FIH1, HIF1AN
Sequence domains: Cupin-like domain
Structure domains:

Ligands and Environments

3 bound ligands:
Ligand FE2 1 x FE2
Ligand SO4 2 x SO4
Ligand HQY 1 x HQY
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: PAL/PLS BEAMLINE 6C1
Spacegroup: P41212
Unit cell:
a: 86.912Å b: 86.912Å c: 144.559Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.259 0.255 0.335
Expression system: Escherichia coli BL21(DE3)

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Citations

1 review citation

Inhibition of 2-oxoglutarate dependent oxygenases.
Rose et al. (2011)
7 other articles