Application | Comment | Organism |
---|---|---|
additional information | LSD1 is a rational target for inducing the reexpression of aberrantly silenced genes | Homo sapiens |
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 | 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 | 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 model | 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 | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
nucleus | - |
Homo sapiens | 5634 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
[histone H3]-N6,N6-dimethyl-L-lysine 4 + 2-oxoglutarate + O2 | Homo sapiens | - |
[histone H3]-N6-methyl-L-lysine 4 + succinate + formaldehyde + CO2 | - |
? | |
[histone H3]-N6-methyl-L-lysine 4 + 2-oxoglutarate + O2 | Homo sapiens | - |
[histone H3]-L-lysine 4 + succinate + formaldehyde + CO2 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O60341 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
colonic adenocarcinoma cell | - |
Homo sapiens | - |
HCT-116 cell | - |
Homo sapiens | - |
RKO cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | the bifunctional enzyme catalyzes the demethylation of H3K9me2/me1 (EC 1.14.11.65) and H3K4me2/me1 | Homo sapiens | ? | - |
? | |
[histone H3]-N6,N6-dimethyl-L-lysine 4 + 2-oxoglutarate + O2 | - |
Homo sapiens | [histone H3]-N6-methyl-L-lysine 4 + succinate + formaldehyde + CO2 | - |
? | |
[histone H3]-N6-methyl-L-lysine 4 + 2-oxoglutarate + O2 | - |
Homo sapiens | [histone H3]-L-lysine 4 + succinate + formaldehyde + CO2 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
KDM1A | - |
Homo sapiens |
LSD1 | - |
Homo sapiens |
lysine-specific demethylase 1 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
FAD | - |
Homo sapiens |
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 |