Inhibitors | Comment | Organism | Structure |
---|---|---|---|
L-alanyl-L-arginyl-L-threonyl-6-(aziridin-1-yl)norleucyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine | compound 2 decomposes when lyophilized to dryness | Homo sapiens | |
L-alanyl-L-arginyl-L-threonyl-6-hydroxynorleucyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine | a peptide containing an oxa-analogue of lysine at the fourth position of a 21 amino acid N-terminal histone H3 tail | Homo sapiens | |
L-alanyl-L-arginyl-L-threonyl-6-[(methylsulfonyl)oxy]norleucyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine | mesylate peptide | Homo sapiens | |
L-alanyl-L-arginyl-L-threonyl-N6-(prop-2-yn-1-yl)lysyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine | a propargyl-Lys-derivatized peptide, MALDI-TOF spectrum of inhibitor-FAD conjugate, the reduced FAD (FADH2) undergoes nucleophilic attack on the propargylic imine and creates the covalent adduct | Homo sapiens | |
additional information | inhibitor synthesis and proposed inactivation mechanism of LSD1, overview | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | dissociation constant for substrate H3K4me2 peptide 3-21 is 0.080 mM | Homo sapiens | |
0.2 | - |
H3K4me2 peptide 3-21 | pH not specified in the publication, 25°C | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
nucleus | - |
Homo sapiens | 5634 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
[histone H3]-N6,N6-dimethyl-L-lysine 4 + 2-oxoglutarate + O2 | Homo sapiens | - |
[histone H3]-N6-methyl-L-lysine 4 + succinate + formaldehyde + CO2 | - |
? | |
[histone H3]-N6-methyl-L-lysine 4 + 2-oxoglutarate + O2 | Homo sapiens | - |
[histone H3]-L-lysine 4 + succinate + formaldehyde + CO2 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O60341 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
H3K4me2 peptide 3-21 + 2-oxoglutarate + O2 | - |
Homo sapiens | H3K4me1 peptide 3-21 + succinate + formaldehyde + CO2 | - |
? | |
additional information | the bifunctional enzyme catalyzes the demethylation of H3K4me2/me1 and H3K9me2/me1 (EC 1.14.11.65). LSD1 is specific for Lys-4 of histone H3 and can oxidatively demethylate the dimethyl or monomethyl Lys-containing substrates | Homo sapiens | ? | - |
? | |
[histone H3]-N6,N6-dimethyl-L-lysine 4 + 2-oxoglutarate + O2 | - |
Homo sapiens | [histone H3]-N6-methyl-L-lysine 4 + succinate + formaldehyde + CO2 | - |
? | |
[histone H3]-N6-methyl-L-lysine 4 + 2-oxoglutarate + O2 | - |
Homo sapiens | [histone H3]-L-lysine 4 + succinate + formaldehyde + CO2 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
BHC110 | - |
Homo sapiens |
KDM1A | - |
Homo sapiens |
LSD1 | - |
Homo sapiens |
lysine-specific demethylase-1 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
FAD | dependent on | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics, steady-state progress curves are obtained for the inactivation of LSD1 | Homo sapiens | |
0.0043 | - |
L-alanyl-L-arginyl-L-threonyl-N6-(prop-2-yn-1-yl)lysyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine | pH and temperature not specified in the publication | Homo sapiens | |
0.0156 | - |
L-alanyl-L-arginyl-L-threonyl-6-(aziridin-1-yl)norleucyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine | pH and temperature not specified in the publication | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
evolution | LSD1 belongs to the amine oxidase family which are flavin-dependent enzymes that utilize O2 and generate H2O2 and formaldehyde as byproducts | Homo sapiens |
metabolism | histone modification is a major mechanism of regulation in gene expression, replication, and repair | Homo sapiens |