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Literature summary for 1.14.99.66 extracted from

  • Huang, Y.; Stewart, T.M.; Wu, Y.; Baylin, S.B.; Marton, L.J.; Perkins, B.; Jones, R.J.; Woster, P.M.; Casero, R.A.
    Novel oligoamine analogues inhibit lysine-specific demethylase 1 and induce reexpression of epigenetically silenced genes (2009), Clin. Cancer Res., 15, 7217-7228.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(12E)-N,N'-diethyl-5,10,16,21-tetraazapentacos-12-ene-1,25-diamine
-
Homo sapiens
(13Z)-N,N'-diethyl-6,11,16,21-tetraazahexacos-13-ene-1,26-diamine
-
Homo sapiens
(19E)-N,N'-diethyl-6,12,17,22,27,33-hexaazaoctatriacont-19-ene-1,38-diamine
-
Homo sapiens
(19Z)-N,N'-diethyl-6,12,17,22,27,33-hexaazaoctatriacont-19-ene-1,38-diamine
-
Homo sapiens
(25E)-N,N'-diethyl-5,11,17,23,28,33,39,45-octaazapentacont-25-ene-1,50-diamine
-
Homo sapiens
(25Z)-N,N'-diethyl-6,12,18,23,28,33,39,45-octaazapentacont-25-ene-1,50-diamine
-
Homo sapiens
(2Z)-N-ethyl-N'-[4-[(4-[[(2Z)-4-(ethylamino)but-2-en-1-yl]amino]butyl)amino]butyl]but-2-ene-1,4-diamine
-
Homo sapiens
(2Z)-N-[4-(ethylamino)butyl]-N'-(4-[[4-(ethylamino)butyl]amino]butyl)but-2-ene-1,4-diamine
-
Homo sapiens
3,8,13,18,23-pentaazapentacosan-1-ol
-
Homo sapiens
additional information oligoamine analogues inhibit lysine-specific demethylase 1 and induce reexpression of epigenetically silenced genes, overview. Treatment of HCT-116 colon adenocarcinoma cells in vitro results in increased H3K4 methylation and reexpression of silenced SFRP genes. This reexpression is also accompanied by a decrease in H3K9me2 repressive mark Homo sapiens
N,N'-diethyl-5,11,17,22,27,33-hexaazaoctatriacontane-1,38-diamine
-
Homo sapiens
N,N'-diethyl-5,11,17,23,28,33,39,45-octaazapentacontane-1,50-diamine
-
Homo sapiens
N-ethyl-N'-[[2-([[4-([[2-([[4-(ethylamino)butyl]amino]methyl)cyclopropyl]methyl]amino)butyl]amino]methyl)cyclopropyl]methyl]butane-1,4-diamine
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
histone H3 N6,N6-dimethyl-L-lysine4 + 2-oxoglutarate + O2 Homo sapiens
-
histone H3 N6-methyl-L-lysine4 + succinate + formaldehyde + CO2
-
?
histone H3 N6-methyl-L-lysine4 + 2-oxoglutarate + O2 Homo sapiens
-
histone H3 L-lysine4 + succinate + formaldehyde + CO2
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
colorectal cancer cell
-
Homo sapiens
-
HCT-116 cell BALB c nu/nu athymic nude mice are implanted with the human colorectal cancer HCT-116 cells Homo sapiens
-
RKO cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
histone H3 N6,N6-dimethyl-L-lysine4 + 2-oxoglutarate + O2
-
Homo sapiens histone H3 N6-methyl-L-lysine4 + succinate + formaldehyde + CO2
-
?
histone H3 N6-methyl-L-lysine4 + 2-oxoglutarate + O2
-
Homo sapiens histone H3 L-lysine4 + succinate + formaldehyde + CO2
-
?

Synonyms

Synonyms Comment Organism
LSD1
-
Homo sapiens
lysine-specific demethylase 1
-
Homo sapiens

General Information

General Information Comment Organism
additional information inhibition of LSD1 by oligoamines increases activating H3K4me2 and H3K4me1 marks and decreases repressive H3K9me2 marks at the promoters of reexpressed genes Homo sapiens