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Literature summary for 1.14.11.65 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)

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

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

Inhibitors

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

Localization Comment Organism GeneOntology No. Textmining
chromatin
-
Homo sapiens 785
-
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
-
-

Purification (Commentary)

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

Source Tissue Comment Organism Textmining
colon
-
Homo sapiens
-
colonic cancer cell
-
Homo sapiens
-
HCT-116 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 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

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 [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8.5
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
FAD dependent on Homo sapiens

General Information

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