|
Cat. No. |
CBCRY04 |
|
Background |
Histone
modifications, such as acetylation and methylation, are
important epigenetic marks that regulate diverse biological
processes that use chromatin as the template, including
transcription. Dysregulation of histone acetylation and
methylation leads to the silencing of tumor suppressor genes and
contributes to cancer progression. Inhibitors of enzymes that
catalyze the addition and removal of these epigenetic marks thus
have therapeutic potential for treating cancer. Lysine-specific
demethylase 1 (LSD1) is the first discovered histone lysine
demethylase and, with the help of its cofactor CoREST,
specifically demethylates mono- and dimethylated histone H3
lysine 4 (H3-K4), thus repressing transcription. |
|
Molecular
description |
Protein
Classification |
Oxidoreductase/repressor |
|
Structure
Weight |
101692.78 Da |
|
Polymer |
1 |
|
Molecule |
Lysine-specific
Histone Demethylase 1 |
|
Chain Length |
666 amino acids
|
|
Polymer |
2 |
|
Molecule |
Rest
Corepressor 1 |
|
Chain Length |
235 amino acids |
|
Crystal
Description |
PDB ID |
2UXX |
|
MMDB ID |
59741 |
|
Source |
E.coli |
|
Method |
X-Ray
Diffraction |
|
Resolution |
2.74
Å |
|
Ligand Chemical
Component |
chloride ion,
FA9, glycerol |
|
Gene
information |
Gene Name |
KDM1 |
|
Synonyms |
RP1-184J9.1;
AOF2; BHC110; KIAA0601; LSD1;BRAF35-HDAC complex protein BHC110;
FAD-binding protein BRAF35-HDAC complex, 110 kDa subunit; amine
oxidase (flavin containing) domain 2; lysine-specific histone
demethylase 1; Flavin-containing amine oxidase domain-containing
protein 2; lysine (K)-specific demethylase 1; EC 1.-.-.-; fad
binding protein braf35 hdac complex 110 kda s; amine oxidase
(flavin containing) domain 2 |
|
UniProt ID |
O60341 |
|
GeneID |
23028 |
|
Chromosome
Location |
1p36.12 |
|
Function |
FAD binding;
electron carrier activity; oxidoreductase activity;
transcription factor activity; transcription factor binding |
|
Gene Name |
RCOR1 |
|
Synonyms |
COREST,
KIAA0071, RCOR, protein CoREST, REST corepressor, REST
corepressor |
|
UniProt ID |
Q9UKL0 |
|
GeneID |
23186 |
|
Chromosome
Location |
14q32.31-q32.32 |
|
Function |
DNA binding;
protein binding |
|
Reference |
Yang,
M., Culhane, J.C., Szewczuk, L.M., Jalili, P., Ball,
H.L., Machius, M., Cole, P.A., Yu, H.Structural Basis for the
Inhibition of the Lsd1 Histone Demethylase by the Antidepressant
Trans-2-Phenylcyclopropylamine.Biochemistry, 2007,46: 8058-8065 |
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