Activating Compound | Comment | Organism | Structure |
---|---|---|---|
ascorbate | slightly activating | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
the coding region of human PHD3 DNA is optimized by using synonymous codons according to the code bias of Escherichia coli, expression of soluble and active N-terminally Trx- and C-terminally His-tagged human PHD3 in Escherichia coli strain BL21(DE3)pLysS at lower induction temperature of 25°C | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1,1',1'',1'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetrapropan-2-ol | noncompetitive inhibition | Homo sapiens | |
3,3'-[(pyridin-2-ylmethyl)imino]dipropanenitrile | noncompetitive inhibition | Homo sapiens | |
3,3'-[(pyridin-4-ylimino)bis(propane-3,1-diyliminomethanediyl)]diphenol | noncompetitive inhibition | Homo sapiens | |
3,3'-[(pyridin-4-ylimino)bis[propane-3,1-diylnitrilo(Z)methylylidene]]diphenol | noncompetitive inhibition | Homo sapiens | |
additional information | polynitrogen compound as HIF-1alpha PHD3 inhibitors, the metal complexes of these polynitrogen compounds cannot inhibit the catalytical activity of PHD3, overview. The inhibitory mechanism of PHD3 activity by polynitrogen compounds is due to their binding to iron to form stable coordination complexes | Homo sapiens |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
45000 | - |
x * 45642, recombinant N-terminally Trx- and C-terminally His-tagged enzyme, mass spectrometry, x * 45651, recombinant His-tagged enzyme, mass spectrometry, x * 45000, recombinant His-tagged enzyme, SDS-PAGE | Homo sapiens |
45642 | - |
x * 45642, recombinant N-terminally Trx- and C-terminally His-tagged enzyme, mass spectrometry, x * 45651, recombinant His-tagged enzyme, mass spectrometry, x * 45000, recombinant His-tagged enzyme, SDS-PAGE | Homo sapiens |
45651 | - |
x * 45642, recombinant N-terminally Trx- and C-terminally His-tagged enzyme, mass spectrometry, x * 45651, recombinant His-tagged enzyme, mass spectrometry, x * 45000, recombinant His-tagged enzyme, SDS-PAGE | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2 | Homo sapiens | - |
hypoxia-inducible factor-trans-4-hydroxy-L-proline + succinate + CO2 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
recombinant Trx- and His-tagged enzyme from Escherichia coli strain BL21(DE3)pLysS by nickel affinity chromatography to over 94% purity | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2 | - |
Homo sapiens | hypoxia-inducible factor-trans-4-hydroxy-L-proline + succinate + CO2 | - |
? | |
hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2 | hydroxylation of the proline residue in the HIF-1alpha (556-574) peptide substrate, sequence of residues 556-574: DLDLEMLAPYIPMDDDFQL | Homo sapiens | hypoxia-inducible factor-trans-4-hydroxy-L-proline + succinate + CO2 | - |
? |
Subunits | Comment | Organism |
---|---|---|
? | x * 45642, recombinant N-terminally Trx- and C-terminally His-tagged enzyme, mass spectrometry, x * 45651, recombinant His-tagged enzyme, mass spectrometry, x * 45000, recombinant His-tagged enzyme, SDS-PAGE | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
HIF-1alpha PHD3 | - |
Homo sapiens |
HIF-1alpha prolyl hydroxylase 3 | - |
Homo sapiens |
PHD | - |
Homo sapiens |
prolyl hydroxylase | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics, overview | Homo sapiens | |
0.0253 | - |
3,3'-[(pyridin-4-ylimino)bis[propane-3,1-diylnitrilo(Z)methylylidene]]diphenol | recombinant enzyme, pH 7.0, 37°C | Homo sapiens | |
0.067 | - |
1,1',1'',1'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetrapropan-2-ol | recombinant enzyme, pH 7.0, 37°C | Homo sapiens | |
0.0673 | - |
3,3'-[(pyridin-4-ylimino)bis(propane-3,1-diyliminomethanediyl)]diphenol | recombinant enzyme, pH 7.0, 37°C | Homo sapiens | |
0.0821 | - |
3,3'-[(pyridin-2-ylmethyl)imino]dipropanenitrile | recombinant enzyme, pH 7.0, 37°C | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0128 | - |
recombinant enzyme, pH 7.0, 37°C | Homo sapiens | 3,3'-[(pyridin-4-ylimino)bis(propane-3,1-diyliminomethanediyl)]diphenol | |
0.016 | - |
recombinant enzyme, pH 7.0, 37°C | Homo sapiens | 3,3'-[(pyridin-4-ylimino)bis[propane-3,1-diylnitrilo(Z)methylylidene]]diphenol | |
0.0295 | - |
recombinant enzyme, pH 7.0, 37°C | Homo sapiens | 1,1',1'',1'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetrapropan-2-ol | |
0.0604 | - |
recombinant enzyme, pH 7.0, 37°C | Homo sapiens | 3,3'-[(pyridin-2-ylmethyl)imino]dipropanenitrile |
General Information | Comment | Organism |
---|---|---|
evolution | PHD3 belongs to Fe2+/2-oxoglutarate-dependent oxygenase family | Homo sapiens |
physiological function | prolyl hydroxylases inactivate hypoxia-inducible factor-1alpha by hydroxylation, PHD isozymes play an integral role in oxygen homeostasis. HIF-1alpha is an important regulation factor in the histiocyte under hypoxia conditions | Homo sapiens |