BRENDA - Enzyme Database show
show all sequences of 1.14.11.29

Effects of polynitrogen compounds on the activity of recombinant human HIF-1alpha prolyl hydroxylase 3 in E. coli

Geng, Z.; Zhu, J.; Cao, J.; Geng, J.; Song, X.; Zhang, Z.; Bian, N.; Wang, Z.; J. Inorg. Biochem. 105, 391-399 (2011)

Data extracted from this reference:

Activating Compound
Activating Compound
Commentary
Organism
Structure
ascorbate
slightly activating
Homo sapiens
Cloned(Commentary)
Commentary
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
Commentary
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]
Commentary
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
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2
Homo sapiens
-
hypoxia-inducible factor-trans-4-hydroxy-L-proline + succinate + CO2
-
-
?
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Homo sapiens
-
-
-
Purification (Commentary)
Commentary
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
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2
-
725644
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
725644
Homo sapiens
hypoxia-inducible factor-trans-4-hydroxy-L-proline + succinate + CO2
-
-
-
?
Subunits
Subunits
Commentary
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
Temperature Optimum [°C]
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
37
-
assay at
Homo sapiens
pH Optimum
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
7
-
assay at
Homo sapiens
Ki Value [mM]
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
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
Commentary
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
Activating Compound (protein specific)
Activating Compound
Commentary
Organism
Structure
ascorbate
slightly activating
Homo sapiens
Cloned(Commentary) (protein specific)
Commentary
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
IC50 Value (protein specific)
IC50 Value
IC50 Value Maximum
Commentary
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
Inhibitors (protein specific)
Inhibitors
Commentary
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
Ki Value [mM] (protein specific)
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
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
Molecular Weight [Da] (protein specific)
Molecular Weight [Da]
Molecular Weight Maximum [Da]
Commentary
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) (protein specific)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2
Homo sapiens
-
hypoxia-inducible factor-trans-4-hydroxy-L-proline + succinate + CO2
-
-
?
Purification (Commentary) (protein specific)
Commentary
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) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2
-
725644
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
725644
Homo sapiens
hypoxia-inducible factor-trans-4-hydroxy-L-proline + succinate + CO2
-
-
-
?
Subunits (protein specific)
Subunits
Commentary
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
Temperature Optimum [°C] (protein specific)
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
37
-
assay at
Homo sapiens
pH Optimum (protein specific)
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
7
-
assay at
Homo sapiens
General Information
General Information
Commentary
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
General Information (protein specific)
General Information
Commentary
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
Other publictions for EC 1.14.11.29
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
741945
Osipyants
Enzyme–substrate reporters ...
Homo sapiens
Biochemistry
82
1207-1214
2017
-
-
-
-
-
-
4
-
-
-
-
3
-
3
-
-
-
-
-
1
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
12
-
-
-
-
-
3
-
-
-
-
-
3
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
742225
Miikkulainen
HIF prolyl hydroxylase PHD3 r ...
Homo sapiens
Cancer Metab.
5
5-5
2017
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
2
2
-
-
-
742585
Badawi
Relative contribution of prol ...
Homo sapiens
Front. Neurosci.
11
239
2017
-
-
-
-
-
-
1
-
-
-
-
1
-
1
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
743380
Kozlova
Hypoxia-inducible factor prol ...
Homo sapiens
Oncotarget
8
9885-9898
2017
-
-
-
-
-
-
-
-
-
-
-
1
-
2
-
-
-
-
-
2
-
-
1
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
2
-
-
1
1
-
-
-
-
-
-
-
-
-
2
2
-
-
-
741826
Chen
Alternative splicing transcri ...
Megalobrama amblycephala
Biochem. Biophys. Res. Commun.
469
737-742
2016
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
10
-
-
1
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
10
-
-
1
1
-
-
-
-
-
-
-
-
1
1
1
1
-
-
743284
Kapitsinou
The endothelial prolyl-4-hydr ...
Mus musculus
Mol. Cell. Biol.
36
1584-1594
2016
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
1
1
-
-
-
743285
Arsenault
The zinc finger of prolyl hyd ...
Mus musculus
Mol. Cell. Biol.
36
2328-2343
2016
-
-
-
-
-
-
-
-
-
1
-
1
-
3
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
741910
Pektas
Increased turnover at limitin ...
Homo sapiens
Biochemistry
54
2851-2857
2015
-
-
1
-
2
-
-
9
-
-
-
1
-
2
-
-
1
-
-
-
-
-
2
1
-
-
-
9
-
-
-
-
-
-
-
-
-
1
-
-
2
-
-
-
-
9
-
-
-
1
-
-
-
1
-
-
-
-
2
1
-
-
-
9
-
-
-
-
-
-
-
-
8
8
742307
Bishop
HIF hydroxylase pathways in c ...
Homo sapiens
Circ. Res.
117
65-79
2015
-
-
-
-
-
-
2
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
742656
Wang
Current advances in the novel ...
Caenorhabditis elegans, Drosophila melanogaster
Insect Mol. Biol.
24
634-648
2015
-
-
-
-
-
-
-
-
-
-
-
2
-
7
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
2
2
-
-
-
743203
Giannetto
Hypoxia-inducible factor alph ...
Mytilus galloprovincialis
Mar. Biotechnol.
17
768-781
2015
-
-
-
-
-
-
-
-
-
-
-
1
-
7
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
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-
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-
-
-
-
-
-
-
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-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
743581
Chan
Potent and selective triazole ...
Homo sapiens, Mus musculus
PLoS ONE
10
e0132004
2015
-
-
-
2
-
-
16
-
-
-
-
-
-
6
-
-
-
-
-
7
-
-
6
-
-
-
-
-
-
-
-
-
-
-
6
-
-
-
-
3
-
-
6
37
-
-
-
-
-
-
-
-
-
-
-
21
-
-
6
-
-
-
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