1.5.3.13: N1-acetylpolyamine oxidase
This is an abbreviated version!
For detailed information about N1-acetylpolyamine oxidase, go to the full flat file.
Word Map on EC 1.5.3.13
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1.5.3.13
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spermine
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putrescine
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diamine
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ornithine
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oxidases
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n1-acetyltransferase
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s-adenosylmethionine
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n1-acetylspermine
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fad-dependent
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monoamine
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3-aminopropanal
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1,3-diaminopropane
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cadaverine
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apoplastic
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aminoaldehydes
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aminoguanidine
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acrolein
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back-conversion
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alpha-difluoromethylornithine
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samdc
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n1-acetylated
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thermospermine
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norspermidine
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n8-acetylspermidine
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tetraamine
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1.4.3.6
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analysis
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medicine
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pharmacology
- 1.5.3.13
- spermine
- putrescine
-
diamine
- ornithine
- oxidases
-
n1-acetyltransferase
- s-adenosylmethionine
- n1-acetylspermine
-
fad-dependent
-
monoamine
- 3-aminopropanal
- 1,3-diaminopropane
- cadaverine
- apoplastic
- aminoaldehydes
- aminoguanidine
- acrolein
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back-conversion
- alpha-difluoromethylornithine
- samdc
-
n1-acetylated
- thermospermine
- norspermidine
- n8-acetylspermidine
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tetraamine
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1.4.3.6
- analysis
- medicine
- pharmacology
Reaction
Synonyms
APAO, AtPAO5, Bjpao2, EC 1.5.3.11, HPAO, hPAO-1, More, MPAO, N1-acetyl polyamine oxidase, N1-acetylpolyamine oxidase, PAO, PAO5, PAOh1, PAOX, polyamine oxidase, SelPAO5
ECTree
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Inhibitors
Inhibitors on EC 1.5.3.13 - N1-acetylpolyamine oxidase
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1,12-diaminododecane
1,12-diaminododecane derivatives could represent good candidates for the development of novel highly specific mPAO inhibitors
6,6'-[ethane-1,2-diyldi(piperidine-4,1-diyl)]bis[N-[(2-methoxyphenyl)methyl]hexan-1-amine]
17fold selectivity for spermine oxidase over polyamine oxidase
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methoctramine
120fold selectivity for spermine oxidase over polyamine oxidase
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N,N'-butanedienyl butanediamine
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i.e. MDL 72527 or CPC-200, a small molecule specific inhibitor of polyamine oxidase, effectively blocks androgen-induced reactive oxygen species production in human prostate cancer cells, as well as significantly delays prostate cancer progression and death in animals developing spontaneous prostate cancer
N1,N1'-(pentane-1,5-diyl)bis[N6-[(2-methoxyphenyl)methyl]hexane-1,6-diamine]
9fold selectivity for spermine oxidase over polyamine oxidase
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N1,N7-bis(6-[[(2-methoxyphenyl)methyl]amino]hexyl)heptane-1,7-diamine
40fold selectivity for spermine oxidase over polyamine oxidase
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MDL72527
irreversible. In addition to the covalent adduct, a second MDL72527 molecule is bound in the active site. Binding of MDL72527 is accompanied by altered conformations in the APAO backbone
2.5 mM, 70% inhibition of N1-acetylspermine oxidation
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no inhibitory activity: N-(3-aminopropyl)-N-2-propynyl-1,4-butanediamine and N-[3-(2-propynylamino)propyl]-1,4-butanediamine
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additional information
no inhibition at pH 7.5: 1,8-diaminooctane. Comparative study on murine PAO (mPAO) and SMO (mSMO) inhibition. The different behaviour displayed by 1,12-diaminododecane towards mPAO and mSMO reveals the occurrence of basic differences in the ligand binding mode of the two enzymes, the first enzyme interacting mainly with substrate secondary amino groups and the second one with substrate primary amino groups. The data provide the basis for the development of novel and selective inhibitors able to discriminate between mammalian SMO and PAO activities
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additional information
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no inhibition at pH 7.5: 1,8-diaminooctane. Comparative study on murine PAO (mPAO) and SMO (mSMO) inhibition. The different behaviour displayed by 1,12-diaminododecane towards mPAO and mSMO reveals the occurrence of basic differences in the ligand binding mode of the two enzymes, the first enzyme interacting mainly with substrate secondary amino groups and the second one with substrate primary amino groups. The data provide the basis for the development of novel and selective inhibitors able to discriminate between mammalian SMO and PAO activities
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