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Literature summary 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

Application

EC Number Application Comment Organism
1.14.11.65 additional information LSD1 is a rational target for inducing the reexpression of aberrantly silenced genes Homo sapiens
1.14.99.66 additional information LSD1 is a rational target for inducing the reexpression of aberrantly silenced genes Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.14.11.65 gene KDM1A, recombinant expression of N-terminally His-tagged full-length LSD1 protein and deletion mutant DELTA184 LSD1lacking the N-terminal 184 amino acid residues Homo sapiens
1.14.99.66 gene KDM1A, recombinant expression of N-terminally His-tagged full-length LSD1 protein and deletion mutant DELTA184 LSD1lacking the N-terminal 184 amino acid residues Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
1.14.11.65 additional information construction of an enzyme mutant with a deletion of the NH2-terminal 184 amino acid residues (DELTA184 LSD1) Homo sapiens
1.14.99.66 additional information construction of an enzyme mutant with a deletion of the NH2-terminal 184 amino acid residues (DELTA184 LSD1) Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.11.65 (12E)-N,N'-diethyl-5,10,16,21-tetraazapentacos-12-ene-1,25-diamine
-
 Homo sapiens
1.14.11.65 (13Z)-N,N'-diethyl-6,11,16,21-tetraazahexacos-13-ene-1,26-diamine
-
 Homo sapiens
1.14.11.65 (19E)-N,N'-diethyl-6,12,17,22,27,33-hexaazaoctatriacont-19-ene-1,38-diamine i.e PG-11144, exhibits competitive inhibition kinetics at concentrations below 0.010 mmol/l. PG-11144 combined with a DNMT inhibitor increases H3K4 methylation and profoundly inhibits growth of established tumors in vivo Homo sapiens
1.14.11.65 (19Z)-N,N'-diethyl-6,12,17,22,27,33-hexaazaoctatriacont-19-ene-1,38-diamine
-
 Homo sapiens
1.14.11.65 (25E)-N,N'-diethyl-5,11,17,23,28,33,39,45-octaazapentacont-25-ene-1,50-diamine
-
 Homo sapiens
1.14.11.65 (25Z)-N,N'-diethyl-6,12,18,23,28,33,39,45-octaazapentacont-25-ene-1,50-diamine
-
 Homo sapiens
1.14.11.65 (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
1.14.11.65 (2Z)-N-[4-(ethylamino)butyl]-N'-(4-[[4-(ethylamino)butyl]amino]butyl)but-2-ene-1,4-diamine
-
 Homo sapiens
1.14.11.65 3,8,13,18,23-pentaazapentacosan-1-ol
-
 Homo sapiens
1.14.11.65 additional information oligoamine analogues are competitive inhibitors of recombinant LSD1. 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. Use of LSD1 inhibitors in combination with a DNA methyltransferase (DNMT) inhibitors (5-aza-2'-deoxycitidine and 5-azacytidine) is a combination that is not only more efficacious in reactivating specific aberrantly silenced genes but also leads to profound inhibition of the growth of established human colon cancer xenografts in a nude mouse mode Homo sapiens
1.14.11.65 N,N'-diethyl-5,11,17,22,27,33-hexaazaoctatriacontane-1,38-diamine
-
 Homo sapiens
1.14.11.65 N,N'-diethyl-5,11,17,23,28,33,39,45-octaazapentacontane-1,50-diamine
-
 Homo sapiens
1.14.11.65 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
1.14.99.66 (12E)-N,N'-diethyl-5,10,16,21-tetraazapentacos-12-ene-1,25-diamine
-
 Homo sapiens
1.14.99.66 (13Z)-N,N'-diethyl-6,11,16,21-tetraazahexacos-13-ene-1,26-diamine
-
 Homo sapiens
1.14.99.66 (19E)-N,N'-diethyl-6,12,17,22,27,33-hexaazaoctatriacont-19-ene-1,38-diamine i.e PG-11144, exhibits competitive inhibition kinetics at concentrations below 0.010 mmol/l. PG-11144 combined with a DNMT inhibitor increases H3K4 methylation and profoundly inhibits growth of established tumors in vivo Homo sapiens
1.14.99.66 (19Z)-N,N'-diethyl-6,12,17,22,27,33-hexaazaoctatriacont-19-ene-1,38-diamine
-
 Homo sapiens
1.14.99.66 (25E)-N,N'-diethyl-5,11,17,23,28,33,39,45-octaazapentacont-25-ene-1,50-diamine
-
 Homo sapiens
1.14.99.66 (25Z)-N,N'-diethyl-6,12,18,23,28,33,39,45-octaazapentacont-25-ene-1,50-diamine
-
 Homo sapiens
1.14.99.66 (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
1.14.99.66 (2Z)-N-[4-(ethylamino)butyl]-N'-(4-[[4-(ethylamino)butyl]amino]butyl)but-2-ene-1,4-diamine
-
 Homo sapiens
1.14.99.66 3,8,13,18,23-pentaazapentacosan-1-ol
-
 Homo sapiens
1.14.99.66 additional information oligoamine analogues are competitive inhibitors of recombinant LSD1. 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. Use of LSD1 inhibitors in combination with a DNA methyltransferase (DNMT) inhibitors (5-aza-2'-deoxycitidine and 5-azacytidine) is a combination that is not only more efficacious in reactivating specific aberrantly silenced genes but also leads to profound inhibition of the growth of established human colon cancer xenografts in a nude mouse model Homo sapiens
1.14.99.66 N,N'-diethyl-5,11,17,22,27,33-hexaazaoctatriacontane-1,38-diamine
-
 Homo sapiens
1.14.99.66 N,N'-diethyl-5,11,17,23,28,33,39,45-octaazapentacontane-1,50-diamine
-
 Homo sapiens
1.14.99.66 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

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.14.11.65 nucleus
-
 Homo sapiens 5634
-
1.14.99.66 nucleus
-
 Homo sapiens 5634
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.14.11.65 [histone H3]-N6,N6-dimethyl-L-lysine 9 + 2-oxoglutarate + O2 Homo sapiens
-
 [histone H3]-N6-methyl-L-lysine 9 + succinate + formaldehyde + CO2
-
 ?
1.14.11.65 [histone H3]-N6-methyl-L-lysine 9 + 2-oxoglutarate + O2 Homo sapiens
-
 [histone H3]-L-lysine 9 + succinate + formaldehyde + CO2
-
 ?
1.14.99.66 [histone H3]-N6,N6-dimethyl-L-lysine 4 + 2-oxoglutarate + O2 Homo sapiens
-
 [histone H3]-N6-methyl-L-lysine 4 + succinate + formaldehyde + CO2
-
 ?
1.14.99.66 [histone H3]-N6-methyl-L-lysine 4 + 2-oxoglutarate + O2 Homo sapiens
-
 [histone H3]-L-lysine 4 + succinate + formaldehyde + CO2
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.14.11.65 Homo sapiens O60341
-
-
1.14.99.66 Homo sapiens O60341
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.11.65 colonic adenocarcinoma cell
-
 Homo sapiens
-
1.14.11.65 HCT-116 cell
-
 Homo sapiens
-
1.14.11.65 RKO cell
-
 Homo sapiens
-
1.14.99.66 colonic adenocarcinoma cell
-
 Homo sapiens
-
1.14.99.66 HCT-116 cell
-
 Homo sapiens
-
1.14.99.66 RKO cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.11.65 additional information the bifunctional enzyme catalyzes the demethylation of H3K9me2/me1 and H3K4me2/me1 (EC 1.14.99.66) Homo sapiens ?
-
 ?
1.14.11.65 [histone H3]-N6,N6-dimethyl-L-lysine 9 + 2-oxoglutarate + O2
-
 Homo sapiens [histone H3]-N6-methyl-L-lysine 9 + succinate + formaldehyde + CO2
-
 ?
1.14.11.65 [histone H3]-N6-methyl-L-lysine 9 + 2-oxoglutarate + O2
-
 Homo sapiens [histone H3]-L-lysine 9 + succinate + formaldehyde + CO2
-
 ?
1.14.99.66 additional information the bifunctional enzyme catalyzes the demethylation of H3K9me2/me1 (EC 1.14.11.65) and H3K4me2/me1 Homo sapiens ?
-
 ?
1.14.99.66 [histone H3]-N6,N6-dimethyl-L-lysine 4 + 2-oxoglutarate + O2
-
 Homo sapiens [histone H3]-N6-methyl-L-lysine 4 + succinate + formaldehyde + CO2
-
 ?
1.14.99.66 [histone H3]-N6-methyl-L-lysine 4 + 2-oxoglutarate + O2
-
 Homo sapiens [histone H3]-L-lysine 4 + succinate + formaldehyde + CO2
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.14.11.65 KDM1A
-
 Homo sapiens
1.14.11.65 LSD1
-
 Homo sapiens
1.14.11.65 lysine-specific demethylase 1
-
 Homo sapiens
1.14.99.66 KDM1A
-
 Homo sapiens
1.14.99.66 LSD1
-
 Homo sapiens
1.14.99.66 lysine-specific demethylase 1
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.14.11.65 FAD
-
 Homo sapiens
1.14.99.66 FAD
-
 Homo sapiens

General Information

EC Number General Information Comment Organism
1.14.11.65 malfunction treatment of HCT-116 colon adenocarcinoma cells with oligoamine analogues inhibitors 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
1.14.99.66 malfunction treatment of HCT-116 colon adenocarcinoma cells with oligoamine analogues inhibitors 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