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Literature summary for 2.3.1.48 extracted from
- Bisubstrate inhibitors to target histone acetyltransferase 1 (2019), Chem. Biol. Drug Des., 93, 865-873 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in Escherichia coli BL21-CodonPlus (DE3)-RIL cells | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| Ac-L-Lys(CoA)-NH2 | bisubstrate inhibitor | Homo sapiens |  |
| CoA | - |
Homo sapiens | |
| [histone H4]-L-lysine12-CoA | bisubstrate inhibitor, i.e. Ac-SGRGKGGKGLGK(CoA)GGAKRHRK, competitive inhibition with respect to both acetyl-CoA and histone H4, highly specific inhibitor for histone acetyltransferase 1 | Homo sapiens | |
| [histone H4]-L-lysine16-CoA | bisubstrate inhibitor, i.e. Ac-SGRGKGGKGLGKGGAK(CoA)RHRK | Homo sapiens | |
| [histone H4]-L-lysine5-CoA | bisubstrate inhibitor, i.e. Ac-SGRGK(CoA)GGKGLGKGGAKRHRK | Homo sapiens | |
| [histone H4]-L-lysine8-CoA | bisubstrate inhibitor, i.e. Ac-SGRGKGGK(CoA)GLGKGGAKRHRK | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00054 | - |
acetyl-CoA | at pH 8.0 and 30°C | Homo sapiens | |
| 0.0081 | - |
SGRGKGGKGLGKGGAKRHRK | at pH 8.0 and 30°C | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| acetyl-CoA + [histone H4]-L-lysine12 | Homo sapiens | - |
CoA + [histone H4]-N6-acetyl-L-lysine12 | - |
? | |
| acetyl-CoA + [histone H4]-L-lysine5 | Homo sapiens | - |
CoA + [histone H4]-N6-acetyl-L-lysine5 | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | O14929 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| Ni-NTA resin column chromatography | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| acetyl-CoA + SGRGKGGKGLGKGGAKRHRK | - |
Homo sapiens | CoA + SGRGKGGKGLGKGGAKRHR(acK) | - |
? | |
| acetyl-CoA + [histone H4]-L-lysine12 | - |
Homo sapiens | CoA + [histone H4]-N6-acetyl-L-lysine12 | - |
? | |
| acetyl-CoA + [histone H4]-L-lysine5 | - |
Homo sapiens | CoA + [histone H4]-N6-acetyl-L-lysine5 | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Hat1 | - |
Homo sapiens |
| histone acetyltransferase 1 | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0000011 | - |
[histone H4]-L-lysine12-CoA | at pH 8.0 and 30°C | Homo sapiens | |
| 0.000022 | - |
[histone H4]-L-lysine5-CoA | at pH 8.0 and 30°C | Homo sapiens | |
| 0.00092 | - |
[histone H4]-L-lysine8-CoA | at pH 8.0 and 30°C | Homo sapiens | |
| 0.0025 | - |
[histone H4]-L-lysine16-CoA | at pH 8.0 and 30°C | Homo sapiens | |
| 0.0146 | - |
CoA | at pH 8.0 and 30°C | Homo sapiens | |
| 0.0262 | - |
Ac-L-Lys(CoA)-NH2 | at pH 8.0 and 30°C | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000023 | - |
at pH 8.0 and 30°C | Homo sapiens | [histone H4]-L-lysine12-CoA | |
| 0.000083 | - |
at pH 8.0 and 30°C | Homo sapiens | [histone H4]-L-lysine5-CoA | |
| 0.0026 | - |
at pH 8.0 and 30°C | Homo sapiens | [histone H4]-L-lysine8-CoA | |
| 0.0072 | - |
at pH 8.0 and 30°C | Homo sapiens | [histone H4]-L-lysine16-CoA | |
| 0.0415 | - |
at pH 8.0 and 30°C | Homo sapiens | CoA | |
| 0.0749 | - |
at pH 8.0 and 30°C | Homo sapiens | Ac-L-Lys(CoA)-NH2 | |
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Release 2023.1 (January 2023)
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