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Literature summary for 1.14.11.65 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
Search for more literature for 1.14.11.65

Application

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

Cloned(Commentary)

Cloned (Comment) Organism
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

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

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 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
(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 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
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

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus
-
 Homo sapiens 5634
-

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens O60341
-
-

Source Tissue

Source Tissue Comment Organism Textmining
colonic adenocarcinoma cell
-
 Homo sapiens
-
HCT-116 cell
-
 Homo sapiens
-
RKO cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
KDM1A
-
 Homo sapiens
LSD1
-
 Homo sapiens
lysine-specific demethylase 1
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
FAD
-
 Homo sapiens

General Information

General Information Comment Organism
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