FIH-1 is an asparaginyl hydroxylase enzyme that regulates the transcriptional activity of hypoxia-inducible factor.

Article Details

Citation

Lando D, Peet DJ, Gorman JJ, Whelan DA, Whitelaw ML, Bruick RK

FIH-1 is an asparaginyl hydroxylase enzyme that regulates the transcriptional activity of hypoxia-inducible factor.

Genes Dev. 2002 Jun 15;16(12):1466-71.

PubMed ID
12080085 [ View in PubMed
]
Abstract

Mammalian cells adapt to hypoxic conditions through a transcriptional response pathway mediated by the hypoxia-inducible factor, HIF. HIF transcriptional activity is suppressed under normoxic conditions by hydroxylation of an asparagine residue within its C-terminal transactivation domain, blocking association with coactivators. Here we show that the protein FIH-1, previously shown to interact with HIF, is an asparaginyl hydroxylase. Like known hydroxylase enzymes, FIH-1 is an Fe(II)-dependent enzyme that uses molecular O(2) to modify its substrate. Together with the recently discovered prolyl hydroxylases that regulate HIF stability, this class of oxygen-dependent enzymes comprises critical regulatory components of the hypoxic response pathway.

DrugBank Data that Cites this Article

Polypeptides
NameUniProt ID
Hypoxia-inducible factor 1-alphaQ16665Details
Hypoxia-inducible factor 1-alpha inhibitorQ9NWT6Details