2.5.1.46: deoxyhypusine synthase
This is an abbreviated version!
For detailed information about deoxyhypusine synthase, go to the full flat file.
Word Map on EC 2.5.1.46
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2.5.1.46
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polyamine
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gc7
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homospermidine
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pyrrolizidine
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n1-guanyl-1,7-diaminoheptane
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nepsilon-4-amino-2-hydroxybutyllysine
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aminobutylation
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hypusine-containing
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1,7-diaminoheptane
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deoxyhypusine-containing
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butylamine
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polyamine-derived
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eif-4d
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medicine
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1,3-diaminopropane
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triamine
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wolff
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drug development
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analysis
- 2.5.1.46
- polyamine
- gc7
- homospermidine
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pyrrolizidine
- n1-guanyl-1,7-diaminoheptane
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nepsilon-4-amino-2-hydroxybutyllysine
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aminobutylation
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hypusine-containing
- 1,7-diaminoheptane
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deoxyhypusine-containing
- butylamine
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polyamine-derived
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eif-4d
- medicine
- 1,3-diaminopropane
- triamine
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wolff
- drug development
- analysis
Reaction
Synonyms
CpDHS, deoxyhypusine synthase, deoxyhypusine synthase (Caulobacter crescentus gene CC0359), deoxyhypusine synthase (Halobacterium strain NRC-1 gene dhs), deoxyhypusine synthase (human clone 30649 gene DHPS subunit reduced), deoxyhypusine synthase (Nicotiana tabacum gene DHS1), deoxyhypusine synthase (Senecio vernalis gene DHS1), deoxyhypusinesynthase, DHPS, DHS, DHS1, DHS2, DHS20, DHS34, DHSc, DHSp, DHYS, Dys1, Dys1p, EC 1.1.1.249, HVO 2297, PF3D7_1412600, speY, synthase, deoxyhypusine, TbDHSc, TbDHSp
ECTree
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Inhibitors
Inhibitors on EC 2.5.1.46 - deoxyhypusine synthase
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(4-[[2-(1H-benzimidazol-2-yl)hydrazinylidene]methyl]phenyl)(hydroxy)oxoammonium
55% inhibition
1-amino-7-guanidinoheptane
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competitive, inhibits binding of spermidine to the enzyme
6-bromo-N-(1H-indol-4-yl)-1-benzothiophene-2-carboxamide
the 6'-bromo substituent is necessary for binding to DHPS
8-fluoro-N-[3-(morpholin-4-yl)propyl]-5H-pyrimido[5,4-b]indol-4-amine
23.6% inhibition
GC7
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a specific DHS-inhibitor, inhibits DHS by competitive replacement of its native spermidine substrate. Inhibition of DHS by GC7 induces antiproliferative effects in vitro. The compound shows a strong antiproliferative effect in glioblastoma cell lines in vitro, while normal human astrocytes are not affected, and it causes p53 dependent premature senescence, a permanent cell cycle arrestin U-MG 87 cells
N,N'-bis[3,5-bis[1(aminoiminomethyl)-hydrazoethyl]phenyl]dodecanediamide-tetrahydrochloride
N-(3-aminopropyl)-cis-1,4-diaminocyclohexane
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1 mM, less than 50% inhibition
N-(3-aminopropyl)-trans-1,4-diaminocyclohexane
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1 mM, less than 50% inhibition
N-(7-chloroquinolin-4-yl)-N'-methylpropane-1,3-diamine
12.45% inhibition
N-guanyl-1,7-diaminoheptane
shows only little inhibitory effect on the leishmanial recombinant DHS34
N1-methylspermidine
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inhibits generation of spermidine from [eIF5A-precursor]-deoxyhypusine
N4-(3-aminopropyl)-4-methylpentane-1,4-diamine
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1 mM, less than 50% inhibition
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inhibits generation of spermidine from [eIF5A-precursor]-deoxyhypusine
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inhibition in vitro and in vivo, inhibits germination conidia. Although DHS of wheat, fungus, and human can be equally inhibited by the inhibitor CNI-1493 in vitro, application during infection of wheat and maize flowers results in strong inhibition of the pathogen without interference with kernel development, providing the possibiity to selectively inhibit fungal growth without affecting plant growth
CNI-1493
a compound that inhibits fungal DHS activity without affecting grain development
CNI-1493
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inhibition in vitro. Although DHS of wheat, fungus, and human can be equally inhibited by the inhibitor CNI-1493 in vitro, application during infection of wheat and maize flowers results in strong inhibition of the pathogen without interference with kernel development, providing the possibiity to selectively inhibit fungal growth without affecting plant growth
CNI-1493
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inhibition in vitro. Although DHS of wheat, fungus, and human can be equally inhibited by the inhibitor CNI-1493 in vitro, application during infection of wheat and maize flowers results in strong inhibition of the pathogen without interference with kernel development, providing the possibiity to selectively inhibit fungal growth without affecting plant growth
i.e. GC7, almost complete inhibition at 20 microM in both one-step and two-step assays
N''-guanyl-1,7-diaminoheptane
i.e. GC7. Downregulation of eIF5A through inhibition of deoxyhypusine synthase favors the reversal of the Th1 mediated cellular processes but minimally affects CD8 T-cells. Inhibition of elF5A increases the Treg/Th17 ratio, reduces anti-GAD65 antibody production and islet/beta-cell ER stress that leads to improvement in the endocrine pancreas functionality in a humanized model of T1D. Diabetes onset is delayed
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i.e. CNI-1493
N,N'-bis[3,5-bis[1(aminoiminomethyl)-hydrazoethyl]phenyl]decanediamide-tetrahydrochloride
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i.e. CNI-1493
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i.e. DHSI-15
N,N'-bis[3,5-bis[1(aminoiminomethyl)-hydrazoethyl]phenyl]dodecanediamide-tetrahydrochloride
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i.e. DHSI-15
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inhibits generation of spermidine from [eIF5A-precursor]-deoxyhypusine
GC7, a potent competitive inhibitor of DHS, causes an effective inhibition of infection and growth of Cryptosporidium parvum in human HCT-8 adenocarcinoma cells. Complete inhibition at 0.01 mM
N1-guanyl-1,7-diaminoheptane
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inhibits generation of spermidine from [eIF5A-precursor]-deoxyhypusine
N1-guanyl-1,7-diaminoheptane
GC7, inhibits the activity of TbDHSc-TbDBHSp heterotetrameric complex; GC7, inhibits the activity of TbDHSc-TbDBHSp heterotetrameric complex
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inhibits generation of spermidine from [eIF5A-precursor]-deoxyhypusine
no growth inhibition by alpha-difluoromethylornithine, an inhibitor of polyamine biosynthesis, and (R)-3-methylspermidine, while the the combination of alpha-difluoromethylornithine with a racemate or (S)-3-methylspermidine causes cessation of cell growth. Cells treated with racemic 3-MeSpd accumulat intracellularly mainly (S)-3-methylspermidine, but not DHS substrate (R)-3-methylspermidine, explaining the inability of the racemate to support long-term growth
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additional information
inhibitor screning in an anti-malaria compound collection, a guanyl residue seems to be an important lead structure for inhibition of Theileria parva DHS enzyme
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additional information
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inhibitor screning in an anti-malaria compound collection, a guanyl residue seems to be an important lead structure for inhibition of Theileria parva DHS enzyme
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