Activating Compound | Comment | Organism | Structure |
---|---|---|---|
ascorbate | required, Km: 0.26 mM | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
HIF asparaginyl hydroxylase (FIH), His-FIH, FIH-FLAGHis, FIH-V5His, and GST-FIH polypeptides are expressed in Spodoptera frugiperda Sf9 cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3,4-dihydroxybenzoate | - |
Homo sapiens | |
additional information | the Ki-value for 3-hydroxypyridine-2-carbonylglycine and N-((3-hydroxy-6-chloroquinolin-2-yl)carbonyl)glycine are above 0.3 mM | Homo sapiens | |
oxalylglycine | - |
Homo sapiens | |
Pyridine-2,4-dicarboxylate | - |
Homo sapiens | |
Pyridine-2,5-dicarboxylate | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.025 | - |
2-oxoglutarate | pH 7.8, 37°C, Km-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
0.09 | - |
O2 | pH 7.8, 37°C. The Km of FIH for O2 is about 40% of its atmospheric concentration, Km-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Fe2+ | required, Km: 0.0005 mM | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
hypoxia-inducible factor-L-asparagine + 2-oxoglutarate + O2 | Homo sapiens | the activity of hypoxia-inducible transcription factor HIF, an alphabeta heterodimer that has an essential role in adaptation to low oxygen availability, is regulated by two oxygen-dependent hydroxylation events. Hydroxylation of specific proline residues by HIF prolyl 4-hydroxylases targets the HIF-alpha subunit for proteasomal destruction, whereas hydroxylation of an asparagine in the C-terminal transactivation domain prevents its interaction with the transcriptional coactivator p300 | hypoxia-inducible factor-(3S)-3-hydroxy-L-asparagine + succinate + CO2 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
- |
Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
DESGLPQLTSYDCEVNAPI + 2-oxoglutarate + O2 | hypoxia-inducible factor-1alpha peptide 788-806. 9% of the activity obtained with the 35-amino-acid HIF-1alpha peptide DES35 (DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL) | Homo sapiens | ? | - |
? | |
DESGLPQLTSYDCEVNAPIQGSR + 2-oxoglutarate + O2 | hypoxia-inducible factor-1alpha peptide 788-810. 15% of the activity obtained with the 35-amino-acid HIF-1alpha peptide DES35 (DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL) | Homo sapiens | ? | - |
? | |
DESGLPQLTSYDCEVNAPIQGSRNLLQ + 2-oxoglutarate + O2 | hypoxia-inducible factor-1alpha peptide 788-814. 37% of the activity obtained with the 35-amino-acid HIF-1alpha peptide DES35 (DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL) | Homo sapiens | ? | - |
? | |
DESGLPQLTSYDCEVNAPIQGSRNLLQGEEL + 2-oxoglutarate + O2 | hypoxia-inducible factor-1alpha peptide 788-818. 26% of the activity obtained with the 35-amino-acid HIF-1alpha peptide DES35 (DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL) | Homo sapiens | ? | - |
? | |
DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL + 2-oxoglutarate + O2 | hypoxia-inducible factor-1alpha peptide 788-822 | Homo sapiens | ? | - |
? | |
ESYLLPELTRYDCEVNVPVLGSSTLLQGGDLLRAL + 2-oxoglutarate + O2 | hypoxia-inducible factor-2alpha peptide 832-857. 7% of the activity obtained with the 35-amino-acid HIF-1alpha peptide DES35 (DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL) | Homo sapiens | ? | - |
? | |
hypoxia-inducible factor-L-asparagine + 2-oxoglutarate + O2 | the activity of hypoxia-inducible transcription factor HIF, an alphabeta heterodimer that has an essential role in adaptation to low oxygen availability, is regulated by two oxygen-dependent hydroxylation events. Hydroxylation of specific proline residues by HIF prolyl 4-hydroxylases targets the HIF-alpha subunit for proteasomal destruction, whereas hydroxylation of an asparagine in the C-terminal transactivation domain prevents its interaction with the transcriptional coactivator p300 | Homo sapiens | hypoxia-inducible factor-(3S)-3-hydroxy-L-asparagine + succinate + CO2 | - |
? | |
hypoxia-inducible factor-L-asparagine + 2-oxoglutarate + O2 | the enzyme requires particularly long peptide substrates, so that omission of only a few residues from the N or C terminus of a 35-residue HIF-1alpha sequence markedly reduces its substrate activity. Hydroxylation of two HIF-2alpha peptides is far less efficient than that of the corresponding HIF-1alpha peptides | Homo sapiens | hypoxia-inducible factor-(3S)-3-hydroxy-L-asparagine + succinate + CO2 | - |
? | |
LTRYDCEVNVPVLGSSTLL + O2 | hypoxia-inducible factor-2alpha peptide 839-866. 1% of the activity obtained with the 35-amino-acid HIF-1alpha peptide DES35 (DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL) | Homo sapiens | ? | - |
? | |
LTSYDCEVNAPIQGSRNLL + 2-oxoglutarate + O2 | hypoxia-inducible factor-1alpha peptide 795-813. 4% of the activity obtained with the 35-amino-acid HIF-1alpha peptide DES35 (DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL) | Homo sapiens | ? | - |
? | |
PSDLACRLLGQSMDESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRALDQVN + 2-oxoglutarate + O2 | hypoxia-inducible factor-1alpha peptide 775-826. 120% of the activity obtained with the 35-amino-acid HIF-1alpha peptide DES35 (DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL) | Homo sapiens | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
dimer | - |
Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
FIH | - |
Homo sapiens |
HIF asparaginyl hydroxylase | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | the catalytic center activities obtained for the enzyme purified by two alternative procedures are 85-135 and 70-120 mol/mol/min, respectively | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.8 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | the Ki-value for 3-hydroxypyridine-2-carbonylglycine and N-((3-Hydroxy-6-chloroquinolin-2-yl)carbonyl)glycine are above 0.3 mM | Homo sapiens | |
0.002 | - |
oxalylglycine | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
0.01 | - |
3,4-dihydroxybenzoate | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
0.03 | - |
Pyridine-2,4-dicarboxylate | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
0.05 | - |
Pyridine-2,5-dicarboxylate | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
0.1 | - |
PSDLACRLLGQSMDESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRALDQVN | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
0.1 | - |
DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
0.16 | - |
ESYLLPELTRYDCEVNVPVLGSSTLLQGGDLLRAL | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens |