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Literature summary for 1.14.11.67 extracted from

  • Longbotham, J.; Chio, C.; Dharmarajan, V.; Trnka, M.; Torres, I.; Goswami, D.; Ruiz, K.; Burlingame, A.; Griffin, P.; Fujimori, D.
    Histone H3 binding to the PHD1 domain of histone demethylase KDM5A enables active site remodeling (2019), Nat. Commun., 10, 94 .
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
histone H3 the in vitro demethylase activity of the enzyme is allosterically enhanced by binding of its product, unmodified histone H3 peptides, to its PHD1 reader domain Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Sf21 insect cells Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0168
-
[acetylated histone H3 21mer]-N6,N6,N6-trimethyl-L-lysine4 in the presence of 0.038 mM unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens
0.0547
-
[acetylated histone H3 21mer]-N6,N6-dimethyl-L-lysine4 in the presence of 0.038 mM unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens
0.0955
-
[acetylated histone H3 21mer]-N6,N6,N6-trimethyl-L-lysine4 in the absence of unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens
0.229
-
[acetylated histone H3 21mer]-N6,N6-dimethyl-L-lysine4 in the absence of unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Fe2+ 0.05 mM used in assay conditions Homo sapiens
K+ 50 mM used in assay conditions Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
[histone H3]-N6,N6,N6-trimethyl-L-lysine4 + 2-oxoglutarate + O2 Homo sapiens
-
[histone H3]-N6,N6-dimethyl-L-lysine4 + succinate + formaldehyde + CO2
-
?
[histone H3]-N6,N6,N6-trimethyl-L-lysine4 + 3 2-oxoglutarate + 3 O2 Homo sapiens overall reaction [histone H3]-L-lysine4 + 3 succinate + 3 formaldehyde + 3 CO2
-
?
[histone H3]-N6,N6-dimethyl-L-lysine4 + 2-oxoglutarate + O2 Homo sapiens
-
[histone H3]-N6-methyl-L-lysine4 + succinate + formaldehyde + CO2
-
?
[histone H3]-N6-methyl-L-lysine4 + 2-oxoglutarate + O2 Homo sapiens
-
[histone H3]-L-lysine4 + succinate + formaldehyde + CO2
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
cobalt resin column chromatography and Superdex S200 gel filtration Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
[acetylated histone H3 21mer]-N6,N6,N6-trimethyl-L-lysine4 + 2-oxoglutarate + O2
-
Homo sapiens [acetylated histone H3 21mer]-N6,N6-dimethyl-L-lysine4 + succinate + formaldehyde + CO2
-
?
[acetylated histone H3 21mer]-N6,N6-dimethyl-L-lysine4 + 2-oxoglutarate + O2
-
Homo sapiens [acetylated histone H3 21mer]-N6-methyl-L-lysine4 + succinate + formaldehyde + CO2
-
?
[histone H3]-N6,N6,N6-trimethyl-L-lysine4 + 2-oxoglutarate + O2
-
Homo sapiens [histone H3]-N6,N6-dimethyl-L-lysine4 + succinate + formaldehyde + CO2
-
?
[histone H3]-N6,N6,N6-trimethyl-L-lysine4 + 3 2-oxoglutarate + 3 O2 overall reaction Homo sapiens [histone H3]-L-lysine4 + 3 succinate + 3 formaldehyde + 3 CO2
-
?
[histone H3]-N6,N6-dimethyl-L-lysine4 + 2-oxoglutarate + O2
-
Homo sapiens [histone H3]-N6-methyl-L-lysine4 + succinate + formaldehyde + CO2
-
?
[histone H3]-N6-methyl-L-lysine4 + 2-oxoglutarate + O2
-
Homo sapiens [histone H3]-L-lysine4 + succinate + formaldehyde + CO2
-
?

Synonyms

Synonyms Comment Organism
KDM5A
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.023
-
[acetylated histone H3 21mer]-N6,N6-dimethyl-L-lysine4 in the absence of unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens
0.023
-
[acetylated histone H3 21mer]-N6,N6-dimethyl-L-lysine4 in the presence of 0.038 mM unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens
0.041
-
[acetylated histone H3 21mer]-N6,N6,N6-trimethyl-L-lysine4 in the presence of 0.038 mM unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens
0.047
-
[acetylated histone H3 21mer]-N6,N6,N6-trimethyl-L-lysine4 in the absence of unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.098
-
[acetylated histone H3 21mer]-N6,N6-dimethyl-L-lysine4 in the absence of unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens
0.43
-
[acetylated histone H3 21mer]-N6,N6-dimethyl-L-lysine4 in the presence of 0.038 mM unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens
0.49
-
[acetylated histone H3 21mer]-N6,N6,N6-trimethyl-L-lysine4 in the absence of unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens
2.43
-
[acetylated histone H3 21mer]-N6,N6,N6-trimethyl-L-lysine4 in the presence of 0.038 mM unmodified histone H3 10mer peptide, at pH 7.5 and 25°C Homo sapiens