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Literature summary for 2.3.1.5 extracted from

  • Liu, L.; Wagner, C.R.; Hanna, P.E.
    Human Arylamine N-Acetyltransferase 1: In Vitro and Intracellular Inactivation by Nitrosoarene Metabolites of Toxic and Carcinogenic Arylamines (2008), Chem. Res. Toxicol., 21, 2005-2016.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens
NAT1 is recombinantly expressed Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-nitrosofluorene potent inactivator, incubation with 2-nitrosofluorene causes 91% inactivation. In the presence of a 500fold excess of glutathione (0.5 mM), inhibition is reduced to 28% Homo sapiens
2-nitrosotoluene less potent inactivator of NAT1, NAT1 with 2-nitrosotoluene causes 46% inhibition of the enzyme, whereas the presence of AcCoA lowers the extent of inhibition to 5% Homo sapiens
4-nitrosobenzene less potent inactivator of NAT1, NAT1 with nitrosobenzene causes 59% inhibition of the enzyme, whereas the presence of AcCoA lowers the extent of inhibition to 13% Homo sapiens
4-nitrosobiphenyl potent inactivator, incubation with 4-nitrosobiphenyl causes 71% inactivation. In the presence of a 500fold excess of glutathione (0.5 mM), inhibition is reduced to 35% Homo sapiens
nitrosobenzene
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
35000
-
HeLa cell NAT1, determined by SDS-PAGE and Western blot analysis Homo sapiens
37000
-
recombinant NAT1, determined by SDS-PAGE and Western blot analysis Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.00161
-
HeLa cell + N-acetyl-L-cysteine + 4-nitrosobiphenyl Homo sapiens
0.00172
-
HeLa cell + 4-nitrosobiphenyl Homo sapiens
0.00408
-
in HeLa cells, substrate: p-aminosalicylic acid Homo sapiens
0.0044
-
in HeLa cells, substrate: p-aminobenzoic acid Homo sapiens
0.00454
-
HeLa cell + N-acetyl-L-cysteine Homo sapiens
0.00466
-
HeLa cell Homo sapiens
0.237
-
recombinant NAT1, substrate: p-aminobenzoic acid Homo sapiens
0.337
-
recombinant NAT1, substrate: p-aminosalicylic acid Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-CoA + 2-aminobenzoic acid
-
Homo sapiens CoA + N-acetyl-2-aminobenzoic acid
-
?
acetyl-CoA + p-aminosalicylic acid
-
Homo sapiens CoA + N-acetyl-4-aminosalicylic acid
-
?

Synonyms

Synonyms Comment Organism
arylamine N-acetyltransferase
-
Homo sapiens
arylamine N-acetyltransferase 1
-
Homo sapiens
NAT1
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at 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
0.00067
-
4-nitrosobiphenyl
-
Homo sapiens
0.00067
-
4-nitrosobiphenyl recombinant NAT1 Homo sapiens
0.54
-
4-nitrosobenzene
-
Homo sapiens
0.54
-
nitrosobenzene recombinant NAT1 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00004
-
-
Homo sapiens 2-nitrosofluorene
0.00004
-
HeLa cell NAT1 Homo sapiens 2-nitrosofluorene
0.00006
-
-
Homo sapiens 4-nitrosobiphenyl
0.00006
-
HeLa cell NAT1 Homo sapiens 4-nitrosobiphenyl
0.091
-
-
Homo sapiens 2-nitrosotoluene
0.091
-
HeLa cell NAT1 Homo sapiens 2-nitrosotoluene
0.237
-
-
Homo sapiens 4-nitrosobenzene
0.237
-
HeLa cell NAT1 Homo sapiens nitrosobenzene