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Literature summary for 2.3.1.5 extracted from
- Allosteric regulation of arylamine N-acetyltransferase 1 by adenosine triphosphate (2018), Biochem. Pharmacol., 158, 153-160 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression in HeLa cell | Homo sapiens |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| modelling predicts that ATP binds within the active site cleft arranged with the triphosphate group in close proximity to arginine 127 | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| K100Q | mutation decreases the potency of ATP as an inhibitor of NAT1. The Hill coefficient increases twofold | Homo sapiens |
| K100R | mutation decreases the potency of ATP as an inhibitor of NAT1. The Hill coefficient increases threefold | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| ATP | non-competitive inhibitor with respect to the acetyl acceptor, competitive inhibitor with respect to acetyl-coenzyme A. There is no effect by presence or absence of Mg2+ | Homo sapiens |  |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.052 | - |
4-Aminobenzoate | presence of 1 mM ATP, 37°C, pH not specified in the publication | Homo sapiens | |
| 0.053 | - |
4-Aminobenzoate | 37°C, pH not specified in the publication | Homo sapiens | |
| 0.242 | - |
acetyl-CoA | 37°C, pH not specified in the publication | Homo sapiens | |
| 0.651 | - |
acetyl-CoA | presence of 1 mM ATP, 37°C, pH not specified in the publication | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P18440 | - |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| acetylation | lysine 100 is a site of posttranslational modification by acetylation | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| acetyl-CoA + 4-aminobenzoate | - |
Homo sapiens | CoA + N-acetyl-4-aminobenzoate | - |
? | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 1.7 | - |
wild-type, 37°C, pH not specified in the publication | Homo sapiens | ATP | |
| 3.8 | - |
mutant K100R, 37°C, pH not specified in the publication | Homo sapiens | ATP | |
| 3.9 | - |
mutant K100Q, 37°C, pH not specified in the publication | Homo sapiens | ATP | |
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Release 2023.1 (January 2023)
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