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Literature summary for 2.3.1.5 extracted from
- Human N-acetyltransferases and drug-induced hepatotoxicity (2008), Curr. Drug Metab., 9, 538-545.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | HIV-infection in human decreases NAT2 activity but not NAT1 | Homo sapiens |
| medicine | NAT is involved in drug induced liver injury. NAT metabolizes drugs causing liver damages: acetylsalicylic acid, dapsone, dihydralazine, isoniazid, p-aminosalicylic acid, procainomide, sulfasalazine, sulfanamide, mesalamine, maprotiline, flutamide | Homo sapiens |
| medicine | NAT2 exerts the effects of drug combinations: NAT2 polymorphisms modify the doxycyline-rifampin interaction that occurs in individuals treated simulataneously with these drugs, that cause an inverse correlation between doxycycline rifampin plasma levels. Among individuals classified as rapid acetylators rifampin plasma levels are greater whereas doxycycline levels are lower, as compared to slow acetylators | Homo sapiens |
| medicine | tobacco smoking is shown to change the risk significance of individual alleles NAT2 to predisposition to multifactor diseases | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| additional information | alleles NAT2*7 in patients indicate slow acetylators the ratio acetyl-INH/INH is 0.93-1.19 opposite 7.4 in patients with NAT2*4/NAT2*4 genotype, but in vitro similar kinetc parameters in NAT2*4 and NAT2*7 for INH are shown (Km (INH): 0.374 nM for NAT2*4 and 0.366 for NAT2*7) | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1-butoxy-2-methylbenzene | - |
Homo sapiens |  |
| 2-butoxyphenol | - |
Homo sapiens | |
| acetoaminophen | - |
Homo sapiens | |
| beta-methylesculetin | inhibits NAT2 but not NAT1 | Homo sapiens | |
| caffeic acid | inhibits NAT1 but not NAT2 | Homo sapiens | |
| curcumin | inhibits NAT2 but not NAT1 | Homo sapiens | |
| ellagic acid | - |
Homo sapiens | |
| ferulic acid | inhibits NAT1 but not NAT2 | Homo sapiens | |
| gallic acid | inhibits NAT1 but not NAT2 | Homo sapiens | |
| glycyrrhizic acid | - |
Homo sapiens | |
| H2O2 | NAT1 is reversibly inactivated by physiological aoncentrations of hydrogen peroxide. Inactivation of NAT1 is fully reversed by physiological concentrations of GSH | Homo sapiens | |
| Ibuprofen | - |
Homo sapiens | |
| kaempferol | inhibits NAT1 and NAT2 | Homo sapiens | |
| Ketoprofen | competitive inhibitor of NAT enzymes | Homo sapiens | |
| luteolin | - |
Homo sapiens | |
| additional information | inhibition profile by polyphenol compounds is different between NAT1 and NAT2. The small polyphenol of cinnamic acid derivates shows some inhibitory activity toward NAT1 , but it has very low activity toward NAT2 | Homo sapiens | |
| paclitaxel | inhibits NAT1 and NAT2 | Homo sapiens | |
| quercetin | inhibits NAT1 and NAT2 | Homo sapiens | |
| vitamin C | - |
Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.366 | - |
isoniazid | in vitro result for allele NAT2*7 | Homo sapiens | |
| 0.374 | - |
isoniazid | in vitro result for allele NAT2*4 | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| breast cancer cell | NAT1 is overexpressed in estrogen receptor-positive breast cancer | Homo sapiens | - |
| embryo | NAT activity is detected in human embryos from first prenatal trimester | Homo sapiens | - |
| liver | NAT activity is found in liver during all life | Homo sapiens | - |
| prostate cancer cell | androgen-dependent expression of NAT1 is demonstrated | Homo sapiens | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| additional information | - |
NAT1 activity is highly regulated by oxidative stress. NAT1 activity is highly sensitive to reactive oxygen or nitrogen species an is reversibly inactivated by H2O2 | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| acetyl-CoA + 8-aminoisoindolo (1,2-b)quinazolin-12(10H)-one | batricylin, an antitumor agent, is shown to be a substrate for NAT2 | Homo sapiens | ? | - |
? | |
| acetyl-CoA + isoniazid | - |
Homo sapiens | CoA + N-acetyl-isoniazid | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| arylamine N-acetyltransferase 1 | - |
Homo sapiens |
| arylamine N-acetyltransferase 2 | - |
Homo sapiens |
| NAT1 | - |
Homo sapiens |
| NAT2 | - |
Homo sapiens |
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