Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.14.99.66 extracted from

  • Culhane, J.C.; Szewczuk, L.M.; Liu, X.; Da, G.; Marmorstein, R.; Cole, P.A.
    A mechanism-based inactivator for histone demethylase LSD1 (2006), J. Am. Chem. Soc., 128, 4536-4537 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
L-alanyl-L-arginyl-L-threonyl-6-(aziridin-1-yl)norleucyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine compound 2 decomposes when lyophilized to dryness Homo sapiens
L-alanyl-L-arginyl-L-threonyl-6-hydroxynorleucyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine a peptide containing an oxa-analogue of lysine at the fourth position of a 21 amino acid N-terminal histone H3 tail Homo sapiens
L-alanyl-L-arginyl-L-threonyl-6-[(methylsulfonyl)oxy]norleucyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine mesylate peptide Homo sapiens
L-alanyl-L-arginyl-L-threonyl-N6-(prop-2-yn-1-yl)lysyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine a propargyl-Lys-derivatized peptide, MALDI-TOF spectrum of inhibitor-FAD conjugate, the reduced FAD (FADH2) undergoes nucleophilic attack on the propargylic imine and creates the covalent adduct Homo sapiens
additional information inhibitor synthesis and proposed inactivation mechanism of LSD1, overview Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information dissociation constant for substrate H3K4me2 peptide 3-21 is 0.080 mM Homo sapiens
0.2
-
H3K4me2 peptide 3-21 pH not specified in the publication, 25°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus
-
Homo sapiens 5634
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
[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

Organism UniProt Comment Textmining
Homo sapiens O60341
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
H3K4me2 peptide 3-21 + 2-oxoglutarate + O2
-
Homo sapiens H3K4me1 peptide 3-21 + succinate + formaldehyde + CO2
-
?
additional information the bifunctional enzyme catalyzes the demethylation of H3K4me2/me1 and H3K9me2/me1 (EC 1.14.11.65). LSD1 is specific for Lys-4 of histone H3 and can oxidatively demethylate the dimethyl or monomethyl Lys-containing substrates 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

Synonyms Comment Organism
BHC110
-
Homo sapiens
KDM1A
-
Homo sapiens
LSD1
-
Homo sapiens
lysine-specific demethylase-1
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
FAD dependent on Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics, steady-state progress curves are obtained for the inactivation of LSD1 Homo sapiens
0.0043
-
L-alanyl-L-arginyl-L-threonyl-N6-(prop-2-yn-1-yl)lysyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine pH and temperature not specified in the publication Homo sapiens
0.0156
-
L-alanyl-L-arginyl-L-threonyl-6-(aziridin-1-yl)norleucyl-L-glutaminyl-L-threonyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-threonylglycylglycyl-L-lysyl-L-alanyl-L-prolyl-L-arginyl-L-lysyl-L-glutaminyl-L-leucyl-L-alanine pH and temperature not specified in the publication Homo sapiens

General Information

General Information Comment Organism
evolution LSD1 belongs to the amine oxidase family which are flavin-dependent enzymes that utilize O2 and generate H2O2 and formaldehyde as byproducts Homo sapiens
metabolism histone modification is a major mechanism of regulation in gene expression, replication, and repair Homo sapiens