Cloned (Comment) | Organism |
---|---|
expression of His6-tagged LSD1 in Escherichia coli strain BL21(DE3) | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1,11-bis-[3-[1-(1,1-diphenylmethyl)thioureado]]-4,8-diazaundecane | 48.9% inhibition at 0.01 mM | Homo sapiens | |
1,11-bis-[3-[1-(2,2-diphenylethyl)thioureado]]-4,8-diazaundecane | 75.2% inhibition at 0.01 mM | Homo sapiens | |
1,11-bis-[3-[1-(3,3-diphenylpropyl)thioureado]]-4,8-diazaundecane | 7.8% inhibition at 0.01 mM | Homo sapiens | |
1,11-bis-[3-[1-(3,3-diphenylpropyl)ureado]]-4,8-diazaundecane | 7.1% inhibition at 0.01 mM | Homo sapiens | |
1,11-bis-[3-[1-(benzyl)thioureado]]-4,8-diazaundecane | 47.9% inhibition at 0.01 mM | Homo sapiens | |
1,11-bis-[3-[1-(benzyl)ureado]]-4,8-diazaundecane | 39.5% inhibition at 0.01 mM | Homo sapiens | |
1,11-bis-[3-[1-(ethyl)thioureado]]-4,8-diazaundecane | 63.8% inhibition at 0.01 mM | Homo sapiens | |
1,11-bis-[3-[1-(ethyl)ureado]]-4,8-diazaundecane | 34.5% inhibition at 0.01 mM | Homo sapiens | |
1,11-bis-[3-[1-(n-propyl)ureado]]-4,8-diazaundecane | 48.7% inhibition at 0.01 mM | Homo sapiens | |
1,11-bis-[5-[1-(N,N-diphenyl)carbamyl]ureado]-4,8-diazaundecane | 8.5% inhibition at 0.01 mM | Homo sapiens | |
1,12-bis-[3-[1-(1,1-diphenylmethyl)thioureado]]-4,9-diazadodecane | 65.6% inhibition at 0.01 mM | Homo sapiens | |
1,12-bis-[3-[1-(2,2-diphenylethyl)thioureado]]-4,9-diazadodecane | 82.9% inhibition at 0.01 mM | Homo sapiens | |
1,12-bis-[3-[1-(3,3-diphenylpropyl)thioureado]]-4,9-diazadodecane | 21.4% inhibition at 0.01 mM | Homo sapiens | |
1,12-bis-[3-[1-(3,3-diphenylpropyl)ureado]]-4,9-diazadodecane | 25.4% inhibition at 0.01 mM | Homo sapiens | |
1,12-bis-[3-[1-(benzyl)ureado]]-4,9-diazadodecane | 50.5% inhibition at 0.01 mM | Homo sapiens | |
1,12-bis-[3-[1-(ethyl)thioureado]]-4,9-diazadodecane | 60% inhibition at 0.01 mM | Homo sapiens | |
1,12-bis-[3-[1-(ethyl)ureado]]-4,9-diazadodecane | 50.8% inhibition at 0.01 mM | Homo sapiens | |
1,12-bis-[3-[1-(n-propyl)thioureado]]-4,9-diazadodecane | 10.4% inhibition at 0.01 mM | Homo sapiens | |
1,12-bis-[3-[1-(n-propyl)ureado]]-4,9-diazadodecane | 21% inhibition at 0.01 mM | Homo sapiens | |
1,12-bis-[5-[1-(N,N-diphenyl)carbamyl]ureado]-4,9-diazadodecane | 73.9% inhibition at 0.01 mM | Homo sapiens | |
1,15-bis-[3-[1-(1,1-diphenylmethyl)thioureado]]-4,12-diazapentadecane | 71.1% inhibition at 0.01 mM | Homo sapiens | |
1,15-bis-[3-[1-(2,2-diphenylethyl)thioureado]]-4,12-diazapentadecane | 80.5% inhibition at 0.01 mM | Homo sapiens | |
1,15-bis-[3-[1-(3,3-diphenylpropyl)thioureado]]-4,12-diazapentadecane | 22.7% inhibition at 0.01 mM | Homo sapiens | |
1,15-bis-[3-[1-(3,3-diphenylpropyl)ureado]]-4,12-diazapentadecane | 48.5% inhibition at 0.01 mM | Homo sapiens | |
1,15-bis-[3-[1-(benzyl)thioureado]]-4,12-diazapentadecane | 64.1% inhibition at 0.01 mM | Homo sapiens | |
1,15-bis-[3-[1-(benzyl)ureado]]-4,12-diazapentadecane | - |
Homo sapiens | |
1,15-bis-[3-[1-(ethyl)ureado]]-4,12-diazapentadecane | - |
Homo sapiens | |
1,15-bis-[3-[1-(n-propyl)ureado]]-4,12-diazapentadecane | 8.5% inhibition at 0.01 mM | Homo sapiens | |
1,15-bis-[5-[1-(N,N-diphenyl)carbamyl]ureado]-4,12-diazapentadecane | 30.0% inhibition at 0.01 mM | Homo sapiens | |
bis-[3-[1-(benzyl)thioureado]]-4,9-diazadodecane | 25.2% inhibition at 0.01 mM | Homo sapiens | |
additional information | (bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators with the potential for use as antitumor agents, overview. No inhibition by 7 and 17, poor inhibition by 11 | Homo sapiens |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
Calu-6 cell | - |
Homo sapiens | - |
lung carcinoma cell | - |
Homo sapiens | - |
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 | Comment | Organism |
---|---|---|
LSD1 | - |
Homo sapiens |
lysine-specific demethylase 1 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8.5 | - |
assay at | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
metabolism | histone methylation is a dynamic process regulated by the addition of methyl groups by histone methyltransferases and removal of methyl groups from mono- and dimethyllysines by lysine specific demethylase 1, LSD1, and from mono-, di, and trimethyllysines by specific JumonjiC, JmjC, domain-containing demethylases | Homo sapiens |
physiological function | LSD1 plays an important role in the epigenetic control of gene expression, and aberrant gene silencing secondary to LSD1 overexpression is thought to contribute to the development of cancer | Homo sapiens |