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Literature summary for 1.14.11.29 extracted from

  • Geng, Z.; Zhu, J.; Cao, J.; Geng, J.; Song, X.; Zhang, Z.; Bian, N.; Wang, Z.
    Effects of polynitrogen compounds on the activity of recombinant human HIF-1alpha prolyl hydroxylase 3 in E. coli (2011), J. Inorg. Biochem., 105, 391-399.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
ascorbate slightly activating Homo sapiens

Cloned(Commentary)

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

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 [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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

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 and Products (Substrate)

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

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

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 [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
assay at Homo sapiens

Ki Value [mM]

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 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

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