Cloned (Comment) | Organism |
---|---|
gene KDM1A, recombinant expression of FLAG-tagged wild-type and mutant enzymes in Escherichia coli strain BL21, recombinant expression of FLAG-tagged wild-type enzyme in Spodoptera frugiperda SF21 cells via baculovrial expression system. Ectopic expression of the LSD1 enzymatically dead mutant K661A | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
K661A | enzymatically dead mutant of BHC110 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | histone deacetylase (HDAC) inhibitors are a promising class of anticancer agents for the treatment of solid and hematological malignancies. HDAC inhibitors diminish histone H3 lysine 4 (H3K4) demethylation by LSD1 in vitro. In vivo analysis reveals an increased H3K4 methylation concomitant with inhibition of nucleosomal deacetylation by HDAC inhibitors. Histone H3K4 demethylation is a secondary target of HDAC inhibitors | Homo sapiens | |
sodium butyrate | a histone deacetylase (HDAC) inhibitor | Homo sapiens | |
trichostatin A | a histone deacetylase (HDAC) inhibitor | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
nucleosome | - |
Homo sapiens | 786 | - |
nucleus | - |
Homo sapiens | 5634 | - |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Fe2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | functional interplay between histone demethylase and histone deacetylase | ? | - |
? | |
[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 | - |
- |
Purification (Comment) | Organism |
---|---|
recombinant FLAG-tagged wild-type and mutant enzymes from Escherichia coli strain BL21 by M2 affinity chromatography, recombinant FLAG-tagged wild-type enzyme from insect Sf21 cells by M2 affinity chromatography | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
HeLa cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | functional interplay between histone demethylase and histone deacetylase | Homo sapiens | ? | - |
? | |
additional information | the bifunctional enzyme catalyzes the demethylation of H3K4me2/me1 and H3K9me2/me1 (EC 1.14.11.65). Functional interplay between histone demethylase and histone deacetylase. The enzymatic activities of the histone demethylase and the deacetylase are intimately linked. The cross talk between the two enzymes is seen only when nucleosomal substrates are used and is mediated through different domains of the CoREST protein (FLAG-tagged CoREST and mutants are recombinantly expressed in HEK-293 cells and Escherichia coli strain BL21). LSD1-HDAC1 complexes display enhanced acetylation activity in presence of CoREST | 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 histone demethylase 1A | UniProt | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
FAD | dependent on | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
evolution | histone methylation can be reversed by several histone demethylases, including PAD4/PADI4, BHC110/LSD1, and JmjC domain-containing demethylases. a family of multiprotein complexes contains histone deacetylase 1/2 (HDAC1/2) and the histone demethylase LSD1 (BHC110). LSD1 demethylates mono- and dimethyl histone H3 lysine 4 (H3K4) and belongs to a family of FAD-dependent polyamine oxidases which use molecular oxygen as an electron acceptor to oxidize an amine group | Homo sapiens |
metabolism | a family of multiprotein complexes contains histone deacetylase 1/2 (HDAC1/2) and the histone demethylase BHC110 (LSD1). Reconstitution of recombinant complexes reveals a functional connection between HDAC1 and BHC110 only when nucleosomal substrates are present. The enzymatic activity of BHC110 is required to achieve optimal deacetylation in vitro. In vivo functional cross talk between the demethylase and deacetylase enzymes is detected. Demethylation of nucleosomes enhances deacetylation | Homo sapiens |