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Literature summary for 1.14.11.29 extracted from

  • Hirsila, M.; Koivunen, P.; Gunzler, V.; Kivirikko, K.I.; Myllyharju, J.
    Characterization of the human prolyl 4-hydroxylases that modify the hypoxia-inducible factor (2003), J. Biol. Chem., 278, 30772-30780.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
ascorbate activates, Km: 0.14 mM Homo sapiens
ascorbate activates, Km: 0.17 mM Homo sapiens
ascorbate activates, Km: 0.18 mM Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression in Spodoptera frugiperda Sf9 cells and Escherichia coli Homo sapiens

Protein Variants

Protein Variants Comment Organism
R367K inactive mutant of HIF-P4H-1 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-carboxy-4-oxo-3,4-dihydro-1,10-phenanthroline
-
Homo sapiens
3-hydroxypyridine-2-carbonyl-glycine
-
Homo sapiens
N-((3-hydroxy-6-chloroquinolin-2-yl)carbonyl)glycine
-
Homo sapiens
oxalylglycine
-
Homo sapiens
Pyridine-2,4-dicarboxylate
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.006
-
DLDLEMLAPYIPMDDDFQLRSFDQ pH 7.8, 37°C Homo sapiens
0.006
-
DALDLEMLAPYISMDDDFQL pH 7.8, 37°C Homo sapiens
0.007
-
DLEMLAPYIPMDDDFQL pH 7.8, 37°C Homo sapiens
0.007
-
DLDLEMLAPYIPMDDDFQL pH 7.8, 37°C Homo sapiens
0.007
-
EMLAPYIPMDDDFQL pH 7.8, 37°C Homo sapiens
0.007
-
DLDLEMLAPYIPMDDDF pH 7.8, 37°C Homo sapiens
0.007
-
DALDLEMLAPYISMDDDFQL pH 7.8, 37°C Homo sapiens
0.008
-
DLDLEMLAPYIPMDDDFQL pH 7.8, 37°C Homo sapiens
0.008
-
DLDLEMLAPYIPMDDDFQLRSFDQ pH 7.8, 37°C Homo sapiens
0.009
-
DLDLEMLAPYIPMDD pH 7.8, 37°C Homo sapiens
0.01
-
DLDLEMLAPAIPMDDDFQL pH 7.8, 37°C Homo sapiens
0.011
-
ELDLETLAPYIPMDGEDFQ pH 7.8, 37°C Homo sapiens
0.014
-
DLEMLAPYIPMDDDFQL pH 7.8, 37°C Homo sapiens
0.015
-
DALDLEMLAPYISMDDDFQL pH 7.8, 37°C Homo sapiens
0.015
-
LAPYIPMDDDFQL pH 7.8, 37°C Homo sapiens
0.02
-
DLDLEMLAPAIPMDDDFQL pH 7.8, 37°C Homo sapiens
0.02
-
DLDLEMLAPGIPMDDDFQL pH 7.8, 37°C Homo sapiens
0.03
-
DLDLEMLAPYIPMD pH 7.8, 37°C Homo sapiens
0.03
-
ELDLETLAPYIPMDGEDFQ pH 7.8, 37°C Homo sapiens
0.035
-
EMLAPYIPMDDDFQL pH 7.8, 37°C Homo sapiens
0.05
-
DLDLEMLAPYIPMDDDF pH 7.8, 37°C Homo sapiens
0.05
-
EMLAPYIPMDD pH 7.8, 37°C Homo sapiens
0.055
-
2-oxoglutarate pH 7.8, 37°C Homo sapiens
0.06
-
2-oxoglutarate pH 7.8, 37°C Homo sapiens
0.06
-
DLDLEMLAPYIPMDD pH 7.8, 37°C Homo sapiens
0.06
-
EPEELAQLAPTPGDAIISLD pH 7.8, 37°C Homo sapiens
0.07
-
DLDLEMLAPYIPMDDDF pH 7.8, 37°C Homo sapiens
0.07
-
EEPDLSCLAPFVDTYDMMQM pH 7.8, 37°C Homo sapiens
0.08
-
EMLAPYIPMDDDFQL pH 7.8, 37°C Homo sapiens
0.1
-
DLDLEMLAPYIPMDD pH 7.8, 37°C Homo sapiens
0.1
-
DLDLEMLAPYIPMD pH 7.8, 37°C Homo sapiens
0.1
-
EPEELAQLAPTPGDAIISLD pH 7.8, 37°C Homo sapiens
0.1
-
EEPDLSCLAPFVDTYDMMQM pH 7.8, 37°C Homo sapiens
0.13
-
DALTLLAPAAGDTIISLFG pH 7.8, 37°C Homo sapiens
0.23
-
O2 pH 7.8, 37°C Homo sapiens
0.25
-
O2 pH 7.8, 37°C Homo sapiens
0.38
-
DALTLLAPAAGDTIISLFG pH 7.8, 37°C 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-(4R)-4-hydroxy-L-proline + succinate + CO2
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens Q9GZT9 HIF-P4H-2
-
Homo sapiens Q9H6Z9 HIF-P4H-3
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
brain expression level of of HIF-P4H-3 mRNA is highest in the adult heart, brain, placenta, lung, and skeletal muscle and in the fetal heart, spleen, and skeletal muscle Homo sapiens
-
brain the level of HIF-P4H-1 mRNA expression is highest in the adult brain, placenta, lung, and kidney Homo sapiens
-
brain the levels of HIF-P4H-2 mRNA expression is highest in the adult heart, brain, lung, and liver and in the fetal brain, heart, spleen, and skeletal muscle Homo sapiens
-
heart expression level of of HIF-P4H-3 mRNA is highest in the adult heart, brain, placenta, lung, and skeletal muscle and in the fetal heart, spleen, and skeletal muscle Homo sapiens
-
heart the levels of HIF-P4H-2 mRNA expression is highest in the adult heart, brain, lung, and liver and in the fetal brain, heart, spleen, and skeletal muscle Homo sapiens
-
kidney the level of HIF-P4H-1 mRNA expression is highest in the adult brain, placenta, lung, and kidney Homo sapiens
-
liver the levels of HIF-P4H-2 mRNA expression is highest in the adult heart, brain, lung, and liver and in the fetal brain, heart, spleen, and skeletal muscle Homo sapiens
-
lung expression level of of HIF-P4H-3 mRNA is highest in the adult heart, brain, placenta, lung, and skeletal muscle and in the fetal heart, spleen, and skeletal muscle Homo sapiens
-
lung the level of HIF-P4H-1 mRNA expression is highest in the adult brain, placenta, lung, and kidney Homo sapiens
-
lung the levels of HIF-P4H-2 mRNA expression is highest in the adult heart, brain, lung, and liver and in the fetal brain, heart, spleen, and skeletal muscle Homo sapiens
-
placenta expression level of of HIF-P4H-3 mRNA is highest in the adult heart, brain, placenta, lung, and skeletal muscle and in the fetal heart, spleen, and skeletal muscle Homo sapiens
-
placenta the level of HIF-P4H-1 mRNA expression is highest in the adult brain, placenta, lung, and kidney Homo sapiens
-
skeletal muscle expression level of of HIF-P4H-3 mRNA is highest in the adult heart, brain, placenta, lung, and skeletal muscle and in the fetal heart, spleen, and skeletal muscle Homo sapiens
-
skeletal muscle the levels of HIF-P4H-2 mRNA expression is highest in the adult heart, brain, lung, and liver and in the fetal brain, heart, spleen, and skeletal muscle Homo sapiens
-
spleen expression level of of HIF-P4H-3 mRNA is highest in the adult heart, brain, placenta, lung, and skeletal muscle and in the fetal heart, spleen, and skeletal muscle Homo sapiens
-
spleen the levels of HIF-P4H-2 mRNA expression is highest in the adult heart, brain, lung, and liver and in the fetal brain, heart, spleen, and skeletal muscle Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
DALDLEMLAPYISMDDDFQL + 2-oxoglutarate + O2 a HIF-3alpha peptide. Vmax is 120% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens ?
-
?
DALDLEMLAPYISMDDDFQL + 2-oxoglutarate + O2 a HIF-3alpha peptide. Vmax is 120% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens DALDLEMLA-((4R)-4-hydroxy-L-proline)-YISMDDDFQL + succinate + CO2
-
?
DALDLEMLAPYISMDDDFQL + 2-oxoglutarate + O2 a HIF-3alpha peptide. Vmax is 150% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens DALDLEMLA-((4R)-4-hydroxy-L-proline)-YISMDDDFQL + succinate + CO2
-
?
DALTLLAPAAGDTIISLFG + 2-oxoglutarate + O2 N-terminal hydroxylation site of HIF-1alpha, Vmax is 100% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens DALTLLA-((4R)-4-hydroxy-L-proline)-AAGDTIISLFG + succinate + CO2
-
?
DALTLLAPAAGDTIISLFG + 2-oxoglutarate + O2 N-terminal hydroxylation site of HIF-1alpha, Vmax is 60% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens DALTLLA-((4R)-4-hydroxy-L-proline)-AAGDTIISLFG + succinate + CO2
-
?
DLDLEMLAPAIPMDDDFQL + 2-oxoglutarate + O2 Vmax is 100% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens DLDLEMLA-((4R)-4-hydroxy-L-proline)-AIPMDDDFQL + succinate + CO2
-
?
DLDLEMLAPGIPMDDDFQL + 2-oxoglutarate + O2 Vmax is 100% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens DLDLEMLA-((4R)-4-hydroxy-L-proline)-GIPMDDDFQL + succinate + CO2
-
?
DLDLEMLAPYIPMD + 2-oxoglutarate + O2 Vmax is 100% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens DLDLEMLA-((4R)-4-hydroxy-L-proline)-YIPMD + succinate + CO2
-
?
DLDLEMLAPYIPMDD + 2-oxoglutarate + O2 Vmax is 100% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens DLDLEMLA-((4R)-4-hydroxy-L-proline)-YIPMDD + succinate + CO2
-
?
DLDLEMLAPYIPMDDDF + 2-oxoglutarate + O2 Vmax is 100% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens DLDLEMLA-((4R)-4-hydroxy-L-proline)-YIPMDDDF + succinate + CO2
-
?
DLDLEMLAPYIPMDDDFQL + 2-oxoglutarate + O2
-
Homo sapiens DLDLEMLA-((4R)-4-hydroxy-L-proline)-YIPMDDDFQL + succinate + CO2
-
?
DLDLEMLAPYIPMDDDFQLRSFDQ + 2-oxoglutarate + O2 Vmax is 100% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens DLDLEMLA-((4R)-4-hydroxy-L-proline)-YIPMDDDFQLRSFDQ + succinate + CO2
-
?
DLEMLAPYIPMDDDFQL + 2-oxoglutarate + O2 Vmax is 100% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens DLEMLA-((4R)-4-hydroxy-L-proline)-YIPMDDDFQL + succinate + CO2
-
?
EEPDLSCLAPFVDTYDMMQM + 2-oxoglutarate + O2 hydroxylation site of Caenorhabditis elegans HIF-alpha. Vmax is 60% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens ?
-
?
EEPDLSCLAPFVDTYDMMQM + 2-oxoglutarate + O2 hydroxylation site of Caenorhabditis elegans HIF-alpha. Vmax is 80% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens ?
-
?
ELDLETLAPYIPMDGEDFQ + 2-oxoglutarate + O2 C-terminal hydroxylation site of HIF-2alpha. Vmax is 100% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens ?
-
?
ELDLETLAPYIPMDGEDFQ + 2-oxoglutarate + O2 C-terminal hydroxylation site of HIF-2alpha. Vmax is 70% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens ?
-
?
ELDLETLAPYIPMDGEDFQ + 2-oxoglutarate + O2 C-terminal hydroxylation site of HIF-2alpha. Vmax is 80% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens ELDLETLA-((4R)-4-hydroxy-L-proline)-YIPMDGEDFQ + succinate + CO2
-
?
EMLAPYIPMDD + 2-oxoglutarate + O2 Vmax is 30% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens EMLA-((4R)-4-hydroxy-L-proline)-YIPMDD + succinate + CO2
-
?
EMLAPYIPMDDDFQL + 2-oxoglutarate + O2 Vmax is 100% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens EMLA-((4R)-4-hydroxy-L-proline)-YIPMDDDFQL + succinate + CO2
-
?
EMLAPYIPMDDDFQL + 2-oxoglutarate + O2 Vmax is 80% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens EMLA-((4R)-4-hydroxy-L-proline)-YIPMDDDFQL + succinate + CO2
-
?
EPEELAQLAPTPGDAIISLD + 2-oxoglutarate + O2 N-terminal hydroxylation site of HIF-2alpha. Vmax is 30% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens ?
-
?
EPEELAQLAPTPGDAIISLD + 2-oxoglutarate + O2 N-terminal hydroxylation site of HIF-2alpha. Vmax is 70% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens ?
-
?
EPEELAQLAPTPGDAIISLD + 2-oxoglutarate + O2 N-terminal hydroxylation site of HIF-2alpha. Vmax is 80% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens ?
-
?
hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2
-
Homo sapiens hypoxia-inducible factor-(4R)-4-hydroxy-L-proline + succinate + CO2
-
?
LAPYIPMDDDFQL + 2-oxoglutarate + O2 Vmax is 90% of the activity with DLDLEMLAPYIPMDDDFQL Homo sapiens LA-((4R)-4-hydroxy-L-proline)-YIPMDDDFQL + succinate + CO2
-
?
additional information the enzyme requires long peptide substrates. No hydroxylation of: Leu-Ala-Pro, Leu-Ala-Pro-Tyr, Leu-Glu-Met-Leu-Ala-Pro, and Leu-Glu-Met-Leu-Ala-Pro-Tyr Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
HIF-P4H-1
-
Homo sapiens
HIF-P4H-2
-
Homo sapiens
HIF-P4H-3
-
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
7.8
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information Ki-values above 0.3 mM: pyridine-2,5-dicarboxylate and 3,4-dihydroxybenzoic acid Homo sapiens
0.0002
-
N-((3-hydroxy-6-chloroquinolin-2-yl)carbonyl)glycine pH 7.8, 37°C Homo sapiens
0.0008
-
N-((3-hydroxy-6-chloroquinolin-2-yl)carbonyl)glycine pH 7.8, 37°C Homo sapiens
0.001
-
3-hydroxypyridine-2-carbonyl-glycine pH 7.8, 37°C Homo sapiens
0.002
-
3-hydroxypyridine-2-carbonyl-glycine pH 7.8, 37°C Homo sapiens
0.007
-
Pyridine-2,4-dicarboxylate pH 7.8, 37°C Homo sapiens
0.008
-
Pyridine-2,4-dicarboxylate pH 7.8, 37°C Homo sapiens
0.008
-
oxalylglycine pH 7.8, 37°C Homo sapiens
0.01
-
oxalylglycine pH 7.8, 37°C Homo sapiens
0.01
-
3-carboxy-4-oxo-3,4-dihydro-1,10-phenanthroline pH 7.8, 37°C Homo sapiens
0.015
-
3-hydroxypyridine-2-carbonyl-glycine pH 7.8, 37°C Homo sapiens
0.03
-
3-carboxy-4-oxo-3,4-dihydro-1,10-phenanthroline pH 7.8, 37°C Homo sapiens
0.04
-
Pyridine-2,4-dicarboxylate pH 7.8, 37°C Homo sapiens
0.05
-
oxalylglycine pH 7.8, 37°C Homo sapiens