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LSD1 with CoREST Protein Crystal

(CBCRY04)  Download Datasheet
Background
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
RCOR1
Synonyms
COREST, KIAA0071, RCOR, protein CoREST, REST corepressor, REST corepressor
UniProt ID
Q9UKL0
Gene ID
23186
Chromosome Location
14q32.31-q32.32
Function
DNA binding; protein binding
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
Gene ID
23028
Chromosome Location
1p36.12
Function
FAD binding; electron carrier activity; oxidoreductase activity; transcription factor activity; transcription factor binding
Reference
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