Cloned (Comment) | Organism |
---|---|
gene KDM1A, recombinant expression of full-length His6-tagged human LSD1 from pET15b bacterial expression vector in Escherichia coli strain BL21(DE3) | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
additional information | LSD1 knockdown by transient siRNA transfection in HCT-116 cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | biguanide and bisguanidine polyamine analogues are potent inhibitors of LSD1. These analogues inhibit LSD1 in human colon carcinoma cells and affect a reexpression of multiple, aberrantly silenced genes important in the development of colon cancer, including members of the secreted frizzle-related proteins (SFRPs) and the GATA family of transcription factors. Reexpression is concurrent with increased H3K4me2 and acetyl-H3K9 marks, decreased H3K9me1 and H3K9me2 repressive marks. Inhibition detection via global H3K4me1 and H3K4me2 levels. HCT116 cells are exposed to increasing concentrations of the indicated compound for 48 h,and 00.03 mg of nuclear protein per lane is analyzed for expression of H3K4me1, H3K4me2, and H3K9me2, overview. Exposure to compounds 1c and 2d produces significant increases in both H3K4me1 and H3K4me2, without affecting global H3K9me2 levels. H3K9me1 and H3K9me2 levels actually decrease in the promoters of the reexpressed genes | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
chromatin | - |
Homo sapiens | 785 | - |
nucleus | - |
Homo sapiens | 5634 | - |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O60341 | - |
- |
Purification (Comment) | Organism |
---|---|
recombinant full-length His6-tagged LSD1 from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and dialysis | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
colon | - |
Homo sapiens | - |
colonic cancer cell | - |
Homo sapiens | - |
HCT-116 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | the bifunctional enzyme catalyzes the demethylation of H3K4me2/me1 (EC 1.14.99.66) and H3K9me2/me1 | 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 | Comment | Organism |
---|---|---|
LSD1 | - |
Homo sapiens |
lysine-specific demethylase 1 | - |
Homo sapiens |
More | see also EC 1.14.99.66 | Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8.5 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
FAD | dependent on | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
malfunction | inhibition of LSD1 by polyamine analogues increases activating H3K4me2 and acetyl H3K9 marks and decreases repressive H3K9me1 and H3K9me2 marks at the promoters of reexpressed genes | Homo sapiens |
physiological function | role of LSD1 in the regulation of gene expression, overview | Homo sapiens |