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Literature summary for 1.14.11.66 extracted from

  • Marmorstein, R.; Trievel, R.C.
    Histone modifying enzymes: structures, mechanisms, and specificities (2009), Biochim. Biophys. Acta, 1789, 58-68.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.14.11.66

Crystallization (Commentary)

Crystallization (Comment) Organism
crystal structures of LSD1/Co-REST complexes bound to histone H3 peptides. LSD1/Co-REST-C complex co-crystallized with a 20-residue histone H3 peptide inhibitor in which Lys4 is mutated to a methionine. Cocrystallization of the enzyme with a suicide inhibitor consisting of a 21-residue histone H3 peptide in which K4 is modified by an N-methylpropargylgroup. Complex structure analysis, overview Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information mutation of R2, Q5, and D555 lead to enzyme inactivation Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Peptide inhibitor a suicide inhibitor consisting of a 21 residue histone H3 peptide in which K4 is modified by an Nmethylpropargyl group. Interactions with the inhibitor include hydrogen bonds to its R2 and Q5 side chains and a salt bridge interaction between the alpha-amine of A1 and Asp555 in LSD1, binding structure, overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens LSD1 is also involved in androgen receptor-dependent demethylation of H3K9me1/2, a methylation site enriched in silent chromatin. The complexes in which LSD1 resides tightly coordinate its gene regulatory functions and also influence its specificity for histone and non-histone substrates ?
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 ?
[histone H3]-N6,N6-dimethyl-L-lysine4 + 2 2-oxoglutarate + 2 O2 Homo sapiens LSD1 represses gene expression through the demethylation of H3K4me1/2, a methylation site frequently associated with transcriptionally poised or active genes, but LSD1 is also linked to gene activation. LSD1 associates with the androgen receptor to enhance the expression of adrogen receptor target genes [histone H3]-L-lysine4 + 2 succinate + 2 formaldehyde + 2 CO2
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 ?
[histone H3]-N6-methyl-L-lysine4 + 2-oxoglutarate + O2 Homo sapiens
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 [histone H3]-L-lysine4 + succinate + formaldehyde + CO2
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 ?
[protein p53]-N6,N6-dimethyl-L-lysine370 + 2-oxoglutarate + O2 Homo sapiens LSD1 demethylates mono- and dimethylated Lys370 in the regulatory domain of the tumor suppressor p53, precluding the binding of the transcriptional coactivator 53BP1 [protein p53]-L-lysine370 + succinate + formaldehyde + CO2
-
 ?
[protein p53]-N6-methyl-L-lysine370 + 2-oxoglutarate + O2 Homo sapiens LSD1 demethylates mono- and dimethylated Lys370 in the regulatory domain of the tumor suppressor p53, precluding the binding of the transcriptional coactivator 53BP1 [protein p53]-L-lysine370 + succinate + formaldehyde + CO2
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens O60341
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-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information LSD1 is also involved in androgen receptor-dependent demethylation of H3K9me1/2, a methylation site enriched in silent chromatin. The complexes in which LSD1 resides tightly coordinate its gene regulatory functions and also influence its specificity for histone and non-histone substrates Homo sapiens ?
-
 ?
additional information aspects of mechanism and specificity of LSD1, overview. To catalyze efficient demethylation, the enzyme requires H3 peptides at least 16 residues in length, consistent with the well-defined electron density corresponding to the first 16 residues of the H3K4M inhibitor. LSD1 exhibits a strong preference toward H3K4me2 substrates lacking other covalent modifications, including R2me, R8me, S10ph, K9ac, and K14ac. The side chains of K9 and K14 are solvent-exposed and do not participate in direct contacts with LSD1 Homo sapiens ?
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 ?
[histone H3]-N6,N6-dimethyl-L-lysine4 + 2 2-oxoglutarate + 2 O2
-
 Homo sapiens [histone H3]-L-lysine4 + 2 succinate + 2 formaldehyde + 2 CO2
-
 ?
[histone H3]-N6,N6-dimethyl-L-lysine4 + 2 2-oxoglutarate + 2 O2 LSD1 represses gene expression through the demethylation of H3K4me1/2, a methylation site frequently associated with transcriptionally poised or active genes, but LSD1 is also linked to gene activation. LSD1 associates with the androgen receptor to enhance the expression of adrogen receptor target genes Homo sapiens [histone H3]-L-lysine4 + 2 succinate + 2 formaldehyde + 2 CO2
-
 ?
[histone H3]-N6-methyl-L-lysine4 + 2-oxoglutarate + O2
-
 Homo sapiens [histone H3]-L-lysine4 + succinate + formaldehyde + CO2
-
 ?
[protein p53]-N6,N6-dimethyl-L-lysine370 + 2-oxoglutarate + O2
-
 Homo sapiens [protein p53]-L-lysine370 + succinate + formaldehyde + CO2
-
 ?
[protein p53]-N6,N6-dimethyl-L-lysine370 + 2-oxoglutarate + O2 LSD1 demethylates mono- and dimethylated Lys370 in the regulatory domain of the tumor suppressor p53, precluding the binding of the transcriptional coactivator 53BP1 Homo sapiens [protein p53]-L-lysine370 + succinate + formaldehyde + CO2
-
 ?
[protein p53]-N6-methyl-L-lysine370 + 2-oxoglutarate + O2
-
 Homo sapiens [protein p53]-L-lysine370 + succinate + formaldehyde + CO2
-
 ?
[protein p53]-N6-methyl-L-lysine370 + 2-oxoglutarate + O2 LSD1 demethylates mono- and dimethylated Lys370 in the regulatory domain of the tumor suppressor p53, precluding the binding of the transcriptional coactivator 53BP1 Homo sapiens [protein p53]-L-lysine370 + succinate + formaldehyde + CO2
-
 ?

Synonyms

Synonyms Comment Organism
BHC110
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 Homo sapiens
KDM1
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 Homo sapiens
KIAA0601
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 Homo sapiens
LSD1
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 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
FAD
-
 Homo sapiens