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Literature summary for 2.3.1.48 extracted from

  • Wapenaar, H.; van der Wouden, P.E.; Groves, M.R.; Rotili, D.; Mai, A.; Dekker, F.J.
    Enzyme kinetics and inhibition of histone acetyltransferase KAT8 (2015), Eur. J. Med. Chem., 105, 289-296.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.3.1.48

Inhibitors

Inhibitors Comment Organism Structure
(4E)-2-(4-acetylphenyl)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-5-methyl-2,4-dihydro-3H-pyrazol-3-one
-
 Homo sapiens
2-(heptylsulfanyl)-1-(2-hydroxyphenyl)ethan-1-one
-
 Homo sapiens
2-butyl-6-hydroxybenzoic acid
-
 Homo sapiens
2-decyl-6-hydroxybenzoic acid 88% inhibition at 0.05 mM Homo sapiens
2-hydroxy-5-pentadecylbenzoic acid 85% inhibition at 0.05 mM Homo sapiens
2-hydroxy-5-pentylbenzoic acid
-
 Homo sapiens
2-hydroxy-6-(11-hydroxyundecyl)benzoic acid
-
 Homo sapiens
2-hydroxy-6-(5-hydroxypentyl)benzoic acid
-
 Homo sapiens
2-hydroxy-6-pentadecylbenzoic acid i.e. anacardic acid, 97% inhibition at 0.05 mM Homo sapiens
5-decyl-2-hydroxybenzoic acid 95% inhibition at 0.05 mM Homo sapiens
anacardic acid
-
 Homo sapiens
additional information no inhibition by 14, 11c, 13, 8a, and 8b; no inhibition by 2-hydroxy-5-pentylbenzoic acid, 2-hydroxy-6-(5-hydroxypentyl)benzoic acid, and (4E)-2-(4-acetylphenyl)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-5-methyl-2,4-dihydro-3H-pyrazol-3-one Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information kinetics and catalytic mechanism of the bi-substrate enzyme KAT8, non-linear Michaelis-Menten regression, overview Homo sapiens
0.0011
-
 acetyl-CoA at 0.015 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
0.0012
-
 acetyl-CoA at 0.030 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
0.0021
-
 acetyl-CoA at 0.060 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
0.0028
-
 acetyl-CoA at 0.090 mM histone H4 peptide, pH and temperature not specified in the publication 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.
acetyl-CoA + histone Homo sapiens
-
 CoA + acetylhistone
-
 ?
acetyl-CoA + histone H4 Homo sapiens acetylation of Lys16 CoA + acetylhistone H4
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q09472
-
-
Homo sapiens Q9H7Z6
-
-

Reaction

Reaction Comment Organism Reaction ID
acetyl-CoA + [protein]-L-lysine = CoA + [protein]-N6-acetyl-L-lysine ping-pong catalytic mechanism of bi-substrate histone acetyltransferase KAT8 Homo sapiens
a

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-CoA + histone
-
 Homo sapiens CoA + acetylhistone
-
 ?
acetyl-CoA + histone
-
 Homo sapiens CoA + acetylhistone in the assay the CoA thiolate is detected by the thiol sensitive fluorescent dye 7-diethylamino-3-(4'-maleimidylphenyl)-4-methylcoumarin ?
acetyl-CoA + histone H4 acetylation of Lys16 Homo sapiens CoA + acetylhistone H4
-
 ?
acetyl-CoA + histone H4 acetylation of Lys16 Homo sapiens CoA + acetylhistone H4 in the assay the CoA thiolate is detected by the thiol sensitive fluorescent dye 7-diethylamino-3-(4'-maleimidylphenyl)-4-methylcoumarin ?
acetyl-CoA + histone H4 peptide a synthetic peptide corresponding to the first 20 amino acids of the histone H4 N-terminus Homo sapiens CoA + acetylhistone H4 peptide
-
 ?

Synonyms

Synonyms Comment Organism
HAT
-
 Homo sapiens
KAT8
-
 Homo sapiens
p300
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.0033
-
 acetyl-CoA at 0.015 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
0.005
-
 acetyl-CoA at 0.030 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
0.012
-
 acetyl-CoA at 0.060 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
0.018
-
 acetyl-CoA at 0.090 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens

Cofactor

Cofactor Comment Organism Structure
acetyl-CoA
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.037
-
 2-decyl-6-hydroxybenzoic acid pH and temperature not specified in the publication Homo sapiens
0.057
-
 5-decyl-2-hydroxybenzoic acid pH and temperature not specified in the publication Homo sapiens
0.064
-
 2-hydroxy-6-pentadecylbenzoic acid pH and temperature not specified in the publication Homo sapiens
0.079
-
 2-hydroxy-5-pentadecylbenzoic acid pH and temperature not specified in the publication Homo sapiens
0.157
-
 2-hydroxy-6-(11-hydroxyundecyl)benzoic acid pH and temperature not specified in the publication Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.32
-
 pH and temperature not specified in the publication Homo sapiens (4E)-2-(4-acetylphenyl)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-5-methyl-2,4-dihydro-3H-pyrazol-3-one

General Information

General Information Comment Organism
evolution histone acetyltransferase KAT8 is a member of the MYST family Homo sapiens
evolution histone acetyltransferase p300 is a member of the p300/CBP family Homo sapiens
physiological function lysine acetyltransferase 8 is a histone acetyltransferase responsible for acetylating lysine 16 on histone H4 and plays a role in cell cycle progression as well as acetylation of the tumor suppressor protein p53 Homo sapiens