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Literature summary for 1.14.11.29 extracted from

  • Nguyen, L.K.; Cavadas, M.A.; Scholz, C.C.; Fitzpatrick, S.F.; Bruning, U.; Cummins, E.P.; Tambuwala, M.M.; Manresa, M.C.; Kholodenko, B.N.; Taylor, C.T.; Cheong, A.
    A dynamic model of the hypoxia-inducible factor 1alpha (HIF-1alpha) network (2013), J. Cell Sci., 126, 1454-1463.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
JNJ1935 a prolyl-hydroxylase selective inhibitor. Low concentrations of JNJ1935 selectively inhibit PHDs, whereas higher concentrations inhibit all hydroxylases, including FIH, EC 1.14.11.30, in vitro and in vivo inhibition Homo sapiens
additional information temporal dynamics of hydroxylase inhibition, overview Homo sapiens
N-(methoxyoxoacetyl)-glycine methyl ester a pan-hydroxylase inhibitor, in vitro and in vivo inhibition Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Fe2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
hypoxia-inducible factor-proline + 2-oxoglutarate + O2 Homo sapiens HIF-1alpha hypoxia-inducible factor-(3S)-3-hydroxy-proline + succinate + CO2
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?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
Homo sapiens
-
Hep-G2 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
hypoxia-inducible factor-proline + 2-oxoglutarate + O2 HIF-1alpha Homo sapiens hypoxia-inducible factor-(3S)-3-hydroxy-proline + succinate + CO2
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?

Synonyms

Synonyms Comment Organism
PHD
-
Homo sapiens
prolyl hydroxylase
-
Homo sapiens

General Information

General Information Comment Organism
malfunction silencing FIH, EC 1.14.11.30, under conditions where prolyl hydroxylase, is inhibited results in increased HIF-1alpha transcriptional activity, but paradoxically decreases HIF-1alpha stability Homo sapiens
metabolism optimal HIF-1alpha transcriptional activity requires sequential inhibition of both prolyl- and asparaginyl-hydroxylases Homo sapiens
additional information modeling of the dynamic regulation of HIF-1alpha transcriptional activity by the hydroxylase. HIF-1alpha stabilisation and transcriptional activity is dependent on oxygen tension Homo sapiens
physiological function key enzyme in activation of the hypoxia-inducible factor (HIF) pathway, a critical step in the transcriptional response to hypoxia. The enzyme is involved in the HIF-1alpha signalling network, overview Homo sapiens