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Literature summary extracted from
- Crystal structure of histone demethylase LSD1 and tranylcypromine at 2.25 A (2008), Biochem. Biophys. Res. Commun., 366, 15-22 .
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 1.14.11.65 | gene lsd1, recombinant expression of GST-tagged enzyme fragment consisting of residues 172-833 in Escherichia coli | Homo sapiens |
| 1.14.99.66 | gene lsd1, recombinant expression of GST-tagged enzyme fragment consisting of residues 172-833 in Escherichia coli | Homo sapiens |
Crystallization (Commentary)
| EC Number | Crystallization (Comment) | Organism |
|---|---|---|
| 1.14.11.65 | recombinant GST-tagged enzyme fragment in complex with inhibitor tranylcypromine, X-ray diffraction structure determination and analysis at 2.25 A resolution | Homo sapiens |
| 1.14.99.66 | 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
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.14.11.65 | additional information | demethylation activity is decreased by other modifications on the H3 tail, such as acetylation and phosphorylation, suggesting possible regulatory mechanisms | Homo sapiens | |
| 1.14.11.65 | 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 |  |
| 1.14.99.66 | additional information | demethylation activity is decreased by other modifications on the H3 tail, such as acetylation and phosphorylation, suggesting possible regulatory mechanisms | Homo sapiens | |
| 1.14.99.66 | 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
| EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|---|
| 1.14.11.65 | nucleosome | - |
Homo sapiens | 786 | - |
| 1.14.99.66 | nucleosome | - |
Homo sapiens | 786 | - |
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 | - |
- |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.14.11.65 | additional information | histone demethylase LSD1 demethylates Lys4 or Lys9 of histone H3 using FAD as cofactor | 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 | additional information | histone demethylase LSD1 demethylates Lys4 or Lys9 of histone H3 using FAD as cofactor | 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 |
| 1.14.99.66 | LSD1 | - |
Homo sapiens |
| 1.14.99.66 | lysine specific demethylase 1 | - |
Homo sapiens |
Cofactor
| EC Number | Cofactor | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.14.11.65 | FAD | essentially required | Homo sapiens | |
| 1.14.99.66 | FAD | essentially required | Homo sapiens | |
General Information
| EC Number | General Information | Comment | Organism |
|---|---|---|---|
| 1.14.11.65 | metabolism | demethylation activity is decreased by other modifications on the H3 tail, such as acetylation and phosphorylation, suggesting possible regulatory mechanisms | Homo sapiens |
| 1.14.11.65 | 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 |
| 1.14.99.66 | metabolism | demethylation activity is decreased by other modifications on the H3 tail, such as acetylation and phosphorylation, suggesting possible regulatory mechanisms | Homo sapiens |
| 1.14.99.66 | physiological function | in non-neural cells, LSD1 removes the transcriptionally active mark of histone H3 Lys4 (H3K4) methyl groups, thereby repressing neuron-specific genes. Recombinant LSD1 alone cannot demethylate nucleosomal H3K4, and CoREST, another component of the complex, is required for the nucleosome-dependent demethylation. LSD1 can act as a transcriptional activator. 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 |
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