Activating Compound | Comment | Organism | Structure |
---|---|---|---|
additional information | interleukin-1beta enhances recruitment of LSD1 to mPGES-1 promoter | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
gene KDM1A, real-time PCR enzyme expression analysis | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
additional information | the enzyme is knocked out by expression of specific siRNA for LSD1 in chondrocytes | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
Pargyline | - |
Homo sapiens | |
tranylcypromine | - |
Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
chromatin | - |
Homo sapiens | 785 | - |
mitochondrion | enzyme LSD1 is present at the proximal region of the microsomal PGES-1 promoter | Homo sapiens | 5739 | - |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Fe2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
histone H3 N6,N6-dimethyl-L-lysine9 + 2-oxoglutarate + O2 | Homo sapiens | - |
histone H3 N6-methyl-L-lysine9 + succinate + formaldehyde + CO2 | - |
? | |
histone H3 N6-methyl-L-lysine9 + 2-oxoglutarate + O2 | Homo sapiens | - |
histone H3 L-lysine9 + succinate + formaldehyde + CO2 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O60341 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
chondrocyte | osteoarthritic chondrocytes | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
histone H3 N6,N6-dimethyl-L-lysine9 + 2-oxoglutarate + O2 | - |
Homo sapiens | histone H3 N6-methyl-L-lysine9 + succinate + formaldehyde + CO2 | - |
? | |
histone H3 N6-methyl-L-lysine9 + 2-oxoglutarate + O2 | - |
Homo sapiens | histone H3 L-lysine9 + succinate + formaldehyde + CO2 | - |
? | |
additional information | histone H3 N6,N6,N6-trimethyl-L-lysine9 is no substrate | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
BHC110 | - |
Homo sapiens |
KDM1A | - |
Homo sapiens |
LSD1 | - |
Homo sapiens |
lysine-specific demethylase 1 | - |
Homo sapiens |
NPAO | - |
Homo sapiens |
p110b | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
FAD | required, LSD1 utilizes FAD as an essential cofactor in catalyzing demethylation of mono- and di-methylated H3K9. Interleukin-1-induced H3K9 demethylation and LSD1 recruitment in human chondrocytes are not associated with significant changes in FAD levels | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
evolution | the enzyme belongs to the superfamily of flavin adenine dinucleotide (FAD)dependent amine oxidases | Homo sapiens |
malfunction | both pharmacological inhibition of LSD1 and small interfering RNA (siRNA) knockdown prevents interleukin 1beta-induced H3K9 demethylation at the mPGES-1 promoter as well as concomitant mPGES-1 protein expression. The level of LSD1 expression is elevated in osteoarthritis cartilage | Homo sapiens |
physiological function | lysine-specific demethylase 1-mediated demethylation of histone H3 lysine 9 contributes to interleukin 1beta-induced microsomal prostaglandin E synthase 1 (mPGES-1) expression in human osteoarthritic chondrocytes. mPGES-1 catalyzes the terminal step in the biosynthesis of PGE2, a critical mediator in the pathophysiology of osteoarthritis. Histone methylation plays an important role in epigenetic gene regulation. LSD1 modulates gene expression through demethylation of either H3K4 or H3K9. H3K9 methylation usually suppresses transcription, whereas H3K4 methylation generally activates transcription. The induction of mPGES-1 expression by interleukin-1beta is associated with decreased levels of mono- and dimethylated H3K9, but not trimethylated H3K9, at the mPGES-1 promoter correlating with the recruitment of the histone demethylase LSD1 | Homo sapiens |