Application | Comment | Organism |
---|---|---|
medicine | the results suggest that the irreversible inactivation of NAT1 by cysplatin may at least partly contribute to the pharmacological and, or toxicological effects of cisplatin | Homo sapiens |
molecular biology | results show that cisplatin inactivates the NAT1 enzyme by forming an adduct with the catalytic cysteine residue of the enzyme | Mus musculus |
molecular biology | results show that cisplatin inactivates the NAT1 enzyme by forming an adduct with the catalytic cysteine residue of the enzyme | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expressed as a His-tagged fusion protein in Escherichia coli | Homo sapiens |
into the pET28a vector for expression in Escherichia coli BL21DE3 cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
cisplatin | exposure of MCF-7 breast cancer cells to cisplatin at clinically relevant concentrations (below 0.4 nM) causes significant dose-dependent inhibition of the endogenous NAT1 enzyme. The incubation of NAT1 with various concentrations of cisplatin results in the dose-dependent modification of cysteine residues, as indicated by the disappearance of fluorescein-conjugated iodoacetamide labeling | Homo sapiens | |
cisplatin | treating C57BL/6J mice with cisplatin significantly decreases murine Nat2 (murine counterpart of human NAT1) enzymatic function in the liver (25% inhibition), kidney (40% inhibition), and blood cells (50% inhibition) | Mus musculus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Mus musculus | - |
- |
- |
Purification (Comment) | Organism |
---|---|
- |
Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
blood | - |
Mus musculus | - |
kidney | - |
Mus musculus | - |
liver | - |
Mus musculus | - |
MCF-7 cell | - |
Homo sapiens | - |
MDA-MB-231 cell | - |
Homo sapiens | - |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
additional information | - |
wild-type enzyme 100% activity, + cisplatin 9%, + AcCoA and cisplatin 13 - 77%, depending on the AcCoA concentration, + CoA and cysplatin 7% | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
acetyl-CoA + 4-aminobenzoic acid | - |
Mus musculus | CoA + N-acetyl-4-aminobenzoic acid | - |
? | |
acetyl-CoA + p-aminobenzoic acid | - |
Homo sapiens | CoA + N-acetyl-4-aminobenzoic acid | - |
? | |
acetyl-CoA + p-aminobenzoic acid | activity assay | Homo sapiens | CoA + N-acetyl-4-aminobenzoic acid | - |
? |
Synonyms | Comment | Organism |
---|---|---|
arylamine N-acetyltransferase 1 | - |
Mus musculus |
arylamine N-acetyltransferase 1 | - |
Homo sapiens |
NAT1 | - |
Mus musculus |
NAT1 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Mus musculus |
37 | - |
assay at | Homo sapiens |
37 | - |
activity assay | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Mus musculus |
7.5 | - |
assay at | Homo sapiens |
7.5 | - |
activity assay | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | the second-order rate constant (kinact) for the inactivation of NAT1 by cisplatin is estimated at 700/M min | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.1 | - |
in MCF-7 breast cancer cells | Homo sapiens | cisplatin | |
0.1 | - |
in MCF7-cells, similar results with MDA-MB-231 cells | Homo sapiens | cisplatin |