1.14.99.29: deoxyhypusine monooxygenase
This is an abbreviated version!
For detailed information about deoxyhypusine monooxygenase, go to the full flat file.
Word Map on EC 1.14.99.29
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1.14.99.29
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eif-5a
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spermidine
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hypusine-containing
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gc7
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mimosine
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ciclopirox
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nepsilon-4-amino-2-hydroxybutyllysine
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drug development
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deferiprone
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eif5a-1
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polyamine-derived
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4-aminobutyl
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diiron
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n1-guanyl-1,7-diaminoheptane
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heat-repeats
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heat-like
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peroxo
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deoxyhypusine-containing
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medicine
- 1.14.99.29
-
eif-5a
- spermidine
-
hypusine-containing
- gc7
- mimosine
- ciclopirox
-
nepsilon-4-amino-2-hydroxybutyllysine
- drug development
- deferiprone
-
eif5a-1
-
polyamine-derived
-
4-aminobutyl
-
diiron
- n1-guanyl-1,7-diaminoheptane
-
heat-repeats
-
heat-like
-
peroxo
-
deoxyhypusine-containing
- medicine
Reaction
Synonyms
deoxyhypusine hydroxylase, deoxyhypusine hydroxylase homologue nero, deoxyhypusine synthase/hydroxylase, deoxyhypusyl hydroxylase, DOHH, DOOH, hDOHH, Lia1, More, nero, oxygenase, deoxyhypusine di-
ECTree
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Inhibitors
Inhibitors on EC 1.14.99.29 - deoxyhypusine monooxygenase
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2-(2-hydroxy-5-methylphenyl)-1,3-thiazole-4-carboxylic acid
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inhibition in vitro and in cells
2-(4-methoxyphenyl)-6-[[2-(4-methoxyphenyl)-3H-benzimidazol-5-yl]methyl]-1H-benzimidazole
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94.1% inhibition at 0.002 mM
alkyl 4-oxo-piperidine 3 carboxylates
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structurally related to dihydropyrimidines, most potent, putative DOHH inhibitors in vitro
deferoxamine
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targets the active metalloenzyme and inhibits DOHH in human vascular endothelial cells
N-phenyl-1-[1-(phenylmethyl)benzimidazol-2-yl]diazenylnaphthalen-2-amine
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87.6% inhibition at 0.002 mM
N-[4-(3,4-diethoxyphenyl)-1,2,5-oxadiazole-3-yl]-3-methylbenzamide
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92.6% inhibition at 0.002 mM
2,2'-dipyridyl
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targets the active metalloenzyme and inhibits DOHH in human vascular endothelial cells
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inhibition in vitro and in cells
2-(2-hydroxy-5-methylphenyl)-4,5-dihydro-1,3-thiazole-4-carboxylic acid
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inhibition in vitro and in cells
ciclopirox
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targets the active metalloenzyme and inhibits DOHH in human vascular endothelial cells
deferiprone
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targets the active metalloenzyme and inhibits DOHH in human vascular endothelial cells
mimosine
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inhibition of enzyme resulting in reduction of steady-state level of transcription initiation factor eIF5A. Effect does not appear to be involved in the modulation of differentiation-related gene 1 expression by mimosine
mimosine
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targets the active metalloenzyme and inhibits DOHH in human vascular endothelial cells
mimosine
synergistic growth inhibition with the combination of miR-331-3p and miR-642-5p and mimosine
mimosine
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inhibits progression of cells from the G1 to S-phase by DOHH inhibition. DOHH reactivation occurs rapidly after inhibitor withdrawal and correlates with synchronized entry into the S-phase. Toxic in vivo
pyridine 2,3-dicarboxylate
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inhibitory effect of pyridine depends on the carboxyl group position
Pyridine 2,4-dicarboxylate
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inhibitory effect of pyridine depends on the carboxyl group position
Pyridine 2,5-dicarboxylate
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inhibitory effect of pyridine depends on the carboxyl group position
Pyridine 3,4-dicarboxylate
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inhibitory effect of pyridine depends on the carboxyl group position
Pyridine 3,5-dicarboxylate
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inhibitory effect of pyridine depends on the carboxyl group position
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a number of metal-chelating inhibitors of DOHH causes growth inhibition and G1 cell cycle arrest in mammalian cells
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additional information
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no inhibition by S-isomers of kojic acid, 3-pyridylalanine, 4-pyridylalanine at 0.3 mM in vitro and at 0.2 mM in cells, no inhibition by 2-(2-aminophenyl)-1,3-thiazole-4-carboxylic acid at 0.4 mM in cells
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additional information
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partial reconstitution of chelator inhibited activity with CuCl2 or Zn(C2H3O2)2
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additional information
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a number of metal-chelating inhibitors of DOHH causes growth inhibition and G1 cell cycle arrest in mammalian cells
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additional information
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design of inhibitors against the human parasite enzyme from Plasmodium falciparum might profit from structural differences and the five HEAT-like repeats present in the parasite DOHH that differ in number and amino acid identity from its human orthologue, which contains four repeats
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additional information
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design of inhibitors against the parasite enzyme might profit from structural differences and the five HEAT-like repeats present in the parasite DOHH that differ in number and amino acid identity from its human orthologue, which contains four repeats. Compounds related structurally to dihydropyrimidines, like the plant amino acid mimosine and the antifungal drug ciclopiroxolamine, are toxic and/or not effective in vivo as anti-malarial drugs in rodents
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additional information
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no inhibition by CuSO4, HgCl2, MgCl2, CdSO4 at 0.005 mM; partial reconstitution of 0.01 mM 1,10-phenanthroline inhibited activity with Co(C2H3O2)2 at 0.03 mM or FeSO4 at 0.005 mM
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additional information
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no inhibition by 2-oxoglutarate, 2-oxoadipinate, 2-oxosuccinate, 3-oxoglutarate, glutarate, malonate, pyruvate
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additional information
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no inhibition at 2 mM N-(2-cyanopropyl)-3-cyanopropylamine
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additional information
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partial reconstitution of 0.01 mM 1,10-phenanthroline inhibited activity with Co(C2H3O2)2 at 0.03 mM or FeSO4 at 0.005 mM
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additional information
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the active site is blocked by two catecholpeptides containing alpha 3,4-dihydroxybenzoyl- and alpha 2,3-dihydroxybenzoyl moiety. The 3,4-dihydroxybenzoyl-containing compound is more potent with a Ki of 32 mM
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