EC Number | Activating Compound | Comment | Organism | Structure |
---|---|---|---|---|
1.14.11.16 | ascorbate | required | Homo sapiens | |
1.14.11.30 | ascorbate | required, Km: 0.26 mM | Homo sapiens |
EC Number | Cloned (Comment) | Organism |
---|---|---|
1.14.11.16 | expressed in Sf9 insect cells as His-tag and GST-fusion protein | Homo sapiens |
1.14.11.30 | HIF asparaginyl hydroxylase (FIH), His-FIH, FIH-FLAGHis, FIH-V5His, and GST-FIH polypeptides are expressed in Spodoptera frugiperda Sf9 cells | Homo sapiens |
EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
1.14.11.16 | additional information | several 2-oxoglutarate analogs inhibits enzyme activity | Homo sapiens | |
1.14.11.30 | 3,4-dihydroxybenzoate | - |
Homo sapiens | |
1.14.11.30 | 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 | |
1.14.11.30 | oxalylglycine | - |
Homo sapiens | |
1.14.11.30 | Pyridine-2,4-dicarboxylate | - |
Homo sapiens | |
1.14.11.30 | Pyridine-2,5-dicarboxylate | - |
Homo sapiens |
EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|---|
1.14.11.16 | 0.025 | - |
2-oxoglutarate | pH 7.8, 30°C | Homo sapiens | |
1.14.11.16 | 0.09 | - |
O2 | pH 7.8, 30°C | Homo sapiens | |
1.14.11.16 | 0.1 | - |
HIF-1alpha peptide Asp788-Leu822 (L-asparagine803) | pH 7.8, 30°C | Homo sapiens | |
1.14.11.30 | 0.025 | - |
2-oxoglutarate | pH 7.8, 37°C, Km-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
1.14.11.30 | 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 |
EC Number | Metals/Ions | Comment | Organism | Structure |
---|---|---|---|---|
1.14.11.16 | Fe2+ | required | Homo sapiens | |
1.14.11.30 | Fe2+ | required, Km: 0.0005 mM | Homo sapiens |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
1.14.11.16 | peptide L-asparagine + 2-oxoglutarate + O2 | Homo sapiens | hydroxylation of Asn803 in hypoxia-inducible transcription factor, converted protein is incapable in interacting with the transcripitonal coactivator p300 | peptide 3-hydroxy-L-asparagine + succinate + CO2 | - |
? | |
1.14.11.30 | 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 | - |
? |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
1.14.11.16 | Homo sapiens | Q9NWT6 | - |
- |
1.14.11.30 | Homo sapiens | - |
- |
- |
EC Number | Purification (Comment) | Organism |
---|---|---|
1.14.11.16 | recombinant enzymes | Homo sapiens |
1.14.11.30 | - |
Homo sapiens |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
1.14.11.16 | HIF-1alpha peptide Asp788-Leu822 (L-Asn803) + 2-oxoglutarate + O2 | much lower activity with peptides lacking residues 819-822, 807-822, and 815-822 | Homo sapiens | HIF-1alpha peptide Asp788-Leu822 (3-hydroxy-L-Asn803) + succinate + CO2 | - |
? | |
1.14.11.16 | HIF-1alpha peptide Asp788-Leu822 (L-asparagine803) + 2-oxoglutarate + O2 | - |
Homo sapiens | ? | - |
r | |
1.14.11.16 | peptide L-asparagine + 2-oxoglutarate + O2 | - |
Homo sapiens | peptide 3-hydroxy-L-asparagine + succinate + CO2 | - |
? | |
1.14.11.16 | peptide L-asparagine + 2-oxoglutarate + O2 | hydroxylation of Asn803 in hypoxia-inducible transcription factor, converted protein is incapable in interacting with the transcripitonal coactivator p300 | Homo sapiens | peptide 3-hydroxy-L-asparagine + succinate + CO2 | - |
? | |
1.14.11.30 | 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 | ? | - |
? | |
1.14.11.30 | 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 | ? | - |
? | |
1.14.11.30 | 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 | ? | - |
? | |
1.14.11.30 | 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 | ? | - |
? | |
1.14.11.30 | DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL + 2-oxoglutarate + O2 | hypoxia-inducible factor-1alpha peptide 788-822 | Homo sapiens | ? | - |
? | |
1.14.11.30 | 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 | ? | - |
? | |
1.14.11.30 | 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 | - |
? | |
1.14.11.30 | 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 | - |
? | |
1.14.11.30 | 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 | ? | - |
? | |
1.14.11.30 | 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 | ? | - |
? | |
1.14.11.30 | 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 | ? | - |
? |
EC Number | Subunits | Comment | Organism |
---|---|---|---|
1.14.11.16 | dimer | homodimer | Homo sapiens |
1.14.11.30 | dimer | - |
Homo sapiens |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
1.14.11.16 | factor inhibiting hypoxia-inducible transcription factor (HIF) | - |
Homo sapiens |
1.14.11.16 | FIH | - |
Homo sapiens |
1.14.11.30 | FIH | - |
Homo sapiens |
1.14.11.30 | HIF asparaginyl hydroxylase | - |
Homo sapiens |
EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|---|
1.14.11.30 | 37 | - |
assay at | Homo sapiens |
EC Number | Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|---|
1.14.11.30 | 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 |
EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|---|
1.14.11.30 | 7.8 | - |
assay at | Homo sapiens |
EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|---|
1.14.11.30 | 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 | |
1.14.11.30 | 0.002 | - |
oxalylglycine | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
1.14.11.30 | 0.01 | - |
3,4-dihydroxybenzoate | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
1.14.11.30 | 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 | |
1.14.11.30 | 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 | |
1.14.11.30 | 0.1 | - |
PSDLACRLLGQSMDESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRALDQVN | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
1.14.11.30 | 0.1 | - |
DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens | |
1.14.11.30 | 0.16 | - |
ESYLLPELTRYDCEVNVPVLGSSTLLQGGDLLRAL | pH 7.8, 37°C, Ki-value is determined using soluble extracts of cells expressing enzyme-FLAGHis | Homo sapiens |