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Literature summary for 1.14.11.29 extracted from

  • Cao, J.; Geng, Z.; Ma, X.; Wen, J.; Yin, Y.; Wang, Z.
    Evidence for inhibition of HIF-1alpha prolyl hydroxylase 3 activity by four biologically active tetraazamacrocycles (2012), Org. Biomol. Chem., 10, 3913-3923.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
ascorbate
-
Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression of His-tagged human PHD3 in Escherichia coli strain BL21(DE3) Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1,1',1'',1'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetrapropan-2-ol chelates Fe2+ in a hexacoordinative mode through four nitrogens of the macrocycle and two oxygens in side arms Homo sapiens
2,2',2'',2'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetamide chelates Fe2+ in a hexacoordinative mode through four nitrogens of the macrocycle and two oxygens in side arms Homo sapiens
3,6,9-tris(naphthalen-1-ylmethyl)-3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene coordinates Fe2+ via triad or tetrad from nitrogen atoms of the parent ring, which leaves vacant position for other ligands binding Homo sapiens
additional information inhibition of the recombinant human PHD3 activity by tetraazamacrocycles, overview Homo sapiens
N,N-dimethyl-5-[3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-trien-6-ylsulfonyl]naphthalen-1-amine coordinates Fe2+ via triad or tetrad from nitrogen atoms of the parent ring, which leaves vacant position for other ligands binding Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information kinetics, overview Homo sapiens
0.067
-
hypoxia-inducible factor-L-proline recombinant enzyme, pH 7.0, 37°C Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Fe2+ dependent on 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 His-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography 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
-
?

Synonyms

Synonyms Comment Organism
HIF-1alpha prolyl hydroxylase 3
-
Homo sapiens
PHD3
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00191
-
3,6,9-tris(naphthalen-1-ylmethyl)-3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene recombinant enzyme, pH 7.0, 37°C Homo sapiens
0.00249
-
N,N-dimethyl-5-[3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-trien-6-ylsulfonyl]naphthalen-1-amine recombinant enzyme, pH 7.0, 37°C Homo sapiens
0.00628
-
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
0.00998
-
2,2',2'',2'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetamide recombinant enzyme, pH 7.0, 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0103
-
recombinant enzyme, pH 7.0, 37°C Homo sapiens 3,6,9-tris(naphthalen-1-ylmethyl)-3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene
0.0207
-
recombinant enzyme, pH 7.0, 37°C Homo sapiens N,N-dimethyl-5-[3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-trien-6-ylsulfonyl]naphthalen-1-amine
0.0309
-
recombinant enzyme, pH 7.0, 37°C Homo sapiens 2,2',2'',2'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetamide
0.0397
-
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