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Literature summary extracted from

  • Huang, Y.; Greene, E.; Murray Stewart, T.; Goodwin, A.C.; Baylin, S.B.; Woster, P.M.; Casero, R.A.
    Inhibition of lysine-specific demethylase 1 by polyamine analogues results in reexpression of aberrantly silenced genes (2007), Proc. Natl. Acad. Sci. USA, 104, 8023-8028 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.14.11.65 gene KDM1A, recombinant expression of full-length His6-tagged human LSD1 from pET15b bacterial expression vector in Escherichia coli strain BL21(DE3) Homo sapiens
1.14.99.66 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

EC Number Protein Variants Comment Organism
1.14.11.65 additional information LSD1 knockdown by transient siRNA transfection in HCT-116 cells Homo sapiens
1.14.99.66 additional information LSD1 knockdown by transient siRNA transfection in HCT-116 cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.11.65 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
1.14.99.66 1,1'-[butane-1,4-diylbis(iminopropane-3,1-diyl)]bis[3-(2,2-diphenylethyl)guanidine]
-
 Homo sapiens
1.14.99.66 1,1'-[butane-1,4-diylbis(iminopropane-3,1-diyl)]bis[3-(3,3-diphenylpropyl)guanidine]
-
 Homo sapiens
1.14.99.66 1,1'-[heptane-1,7-diylbis(iminopropane-3,1-diyl)]bis(3-methylguanidine)
-
 Homo sapiens
1.14.99.66 1,1'-[heptane-1,7-diylbis(iminopropane-3,1-diyl)]bis(3-phenylguanidine)
-
 Homo sapiens
1.14.99.66 1,1'-[propane-1,3-diylbis(iminopropane-3,1-diyl)]bis(2,3-dimethylguanidine)
-
 Homo sapiens
1.14.99.66 1,1'-[propane-1,3-diylbis(iminopropane-3,1-diyl)]bis(3-methylguanidine)
-
 Homo sapiens
1.14.99.66 1,1'-[propane-1,3-diylbis(iminopropane-3,1-diyl)]bis(3-phenylguanidine)
-
 Homo sapiens
1.14.99.66 1,11-bis(N2,N3-dimethyl-N1-guanidino)-4,8-diazaundecane
-
 Homo sapiens
1.14.99.66 1,15-bis(N5-[3,3-(diphenyl)propyl]-N1-biguanido)-4,12-diazapentadecane
-
 Homo sapiens
1.14.99.66 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 Homo sapiens
1.14.99.66 N,N''''-[butane-1,4-diylbis(iminopropane-3,1-diyl)]bis[N'-(2,2-diphenylethyl)(imidodicarbonimidic diamide)]
-
 Homo sapiens
1.14.99.66 N,N''''-[butane-1,4-diylbis(iminopropane-3,1-diyl)]bis[N'-(3,3-diphenylpropyl)(imidodicarbonimidic diamide)]
-
 Homo sapiens
1.14.99.66 N,N''''-[heptane-1,7-diylbis(iminopropane-3,1-diyl)]bis[N'-(2,2-diphenylethyl)(imidodicarbonimidic diamide)]
-
 Homo sapiens
1.14.99.66 N,N''''-[heptane-1,7-diylbis(iminopropane-3,1-diyl)]bis[N'-(3,3-diphenylpropyl)(imidodicarbonimidic diamide)]
-
 Homo sapiens
1.14.99.66 N,N''''-[propane-1,3-diylbis(iminopropane-3,1-diyl)]bis[N'-(2,2-diphenylethyl)(imidodicarbonimidic diamide)]
-
 Homo sapiens
1.14.99.66 N,N''''-[propane-1,3-diylbis(iminopropane-3,1-diyl)]bis[N'-(3,3-diphenylpropyl)(imidodicarbonimidic diamide)]
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.14.11.65 chromatin
-
 Homo sapiens 785
-
1.14.11.65 nucleus
-
 Homo sapiens 5634
-
1.14.99.66 chromatin
-
 Homo sapiens 785
-
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
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.14.11.65 recombinant full-length His6-tagged LSD1 from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and dialysis Homo sapiens
1.14.99.66 recombinant full-length His6-tagged LSD1 from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and dialysis Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.11.65 colon
-
 Homo sapiens
-
1.14.11.65 colonic cancer cell
-
 Homo sapiens
-
1.14.11.65 HCT-116 cell
-
 Homo sapiens
-
1.14.99.66 colon
-
 Homo sapiens
-
1.14.99.66 colonic cancer cell
-
 Homo sapiens
-
1.14.99.66 HCT-116 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 H3K4me2/me1 (EC 1.14.99.66) and H3K9me2/me1 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 H3K4me2 (1-21 aa) peptide + 2-oxoglutarate + O2
-
 Homo sapiens H3K4me1 (1-21 aa) peptide + succinate + formaldehyde + CO2
-
 ?
1.14.99.66 additional information the bifunctional enzyme catalyzes the demethylation of H3K4me2/me1 and H3K9me2/me1 (EC 1.14.11.65) 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 LSD1
-
 Homo sapiens
1.14.11.65 lysine-specific demethylase 1
-
 Homo sapiens
1.14.11.65 More see also EC 1.14.99.66 Homo sapiens
1.14.99.66 LSD1
-
 Homo sapiens
1.14.99.66 lysine-specific demethylase 1
-
 Homo sapiens
1.14.99.66 More see also EC 1.14.11.65 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.14.11.65 37
-
 assay at Homo sapiens
1.14.99.66 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.14.11.65 8.5
-
 assay at Homo sapiens
1.14.99.66 8.5
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.14.11.65 FAD dependent on Homo sapiens
1.14.99.66 FAD dependent on Homo sapiens

General Information

EC Number General Information Comment Organism
1.14.11.65 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
1.14.11.65 physiological function role of LSD1 in the regulation of gene expression, overview Homo sapiens
1.14.99.66 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
1.14.99.66 physiological function dimethyl-lysine 4 histone H3 (H3K4me2) is a transcription-activating chromatin mark at gene promoters, and demethylation of this mark by the lysine-specific demethylase 1 (LSD1), a homologue of polyamine oxidases, broadly represses gene expression. Role of LSD1 in the regulation of gene expression, overview Homo sapiens