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Literature summary for 1.14.11.65 extracted from

  • Mimasu, S.; Sengoku, T.; Fukuzawa, S.; Umehara, T.; Yokoyama, S.
    Crystal structure of histone demethylase LSD1 and tranylcypromine at 2.25 A (2008), Biochem. Biophys. Res. Commun., 366, 15-22 .
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
gene lsd1, recombinant expression of GST-tagged enzyme fragment consisting of residues 172-833 in Escherichia coli Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
recombinant GST-tagged enzyme fragment in complex with inhibitor tranylcypromine, X-ray diffraction structure determination and analysis at 2.25 A resolution Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information demethylation activity is decreased by other modifications on the H3 tail, such as acetylation and phosphorylation, suggesting possible regulatory mechanisms Homo sapiens
tranylcypromine i.e. Parnate, binding structure analysis and modeling, overview. The LSD1-tranylcypromine complex is not completely composed of the five-membered adduct, but partially contains an intermediate. LSD1-flavin is the only place modified by this inhibition Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleosome
-
Homo sapiens 786
-

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
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information histone demethylase LSD1 demethylates Lys4 or Lys9 of histone H3 using FAD as cofactor 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

Cofactor

Cofactor Comment Organism Structure
FAD essentially required Homo sapiens

General Information

General Information Comment Organism
metabolism demethylation activity is decreased by other modifications on the H3 tail, such as acetylation and phosphorylation, suggesting possible regulatory mechanisms Homo sapiens
physiological function LSD1 can act as a transcriptional activator. Androgen receptor and LSD1 form a complex in a ligand-dependent manner and remove the transcriptionally repressive H3K9 methyl groups, thereby de-repressing androgen-receptor-target genes. LSD1 can target different lysine residues and regulate transcription positively or negatively, depending on its binding partners. The large number of LSD1-enriched promoters suggest a broad role in transcriptional regulation for LSD1 Homo sapiens