Page last updated: 2024-10-24

arylamine N-acetyltransferase activity

Definition

Target type: molecularfunction

Catalysis of the reaction: acetyl-CoA + an arylamine = CoA + an N-acetylarylamine. [EC:2.3.1.5]

Arylamine N-acetyltransferase activity is a crucial enzymatic function involved in the detoxification and metabolism of a wide range of endogenous and exogenous compounds. These enzymes, primarily belonging to the NAT family, catalyze the transfer of an acetyl group from acetyl-CoA to the amino group of primary aromatic amines, hydrazines, and other amine-containing molecules. This acetylation process plays a vital role in several cellular processes, including:

* **Detoxification of xenobiotics:** NAT enzymes efficiently detoxify various potentially harmful compounds, including aromatic amines, heterocyclic amines, and drugs, by converting them into less toxic or more water-soluble metabolites, facilitating their excretion.
* **Metabolism of endogenous substrates:** NATs also contribute to the metabolism of endogenous substrates, such as neurotransmitters, hormones, and other bioactive amines. For instance, NAT2, a key enzyme in human drug metabolism, plays a significant role in the acetylation of serotonin, dopamine, and histamine.
* **Regulation of cellular processes:** Acetylation by NATs can alter the activity of various cellular processes, including DNA repair, cell signaling, and immune responses.

The catalytic mechanism of arylamine N-acetyltransferases involves a two-step process. First, the enzyme binds both the acetyl-CoA donor and the amine substrate. Then, the acetyl group is transferred from acetyl-CoA to the amine, forming an acetylated product and releasing CoA. The activity of NAT enzymes is highly dependent on the substrate's chemical structure and the presence of cofactors, particularly acetyl-CoA.

Genetic polymorphisms within the NAT gene family can lead to variations in enzyme activity, influencing individual susceptibility to drug toxicity and the development of certain diseases, highlighting the importance of this enzymatic activity in human health.'
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Proteins (2)

ProteinDefinitionTaxonomy
Arylamine N-acetyltransferase 1An arylamine N-acetyltransferase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P18440]Homo sapiens (human)
Arylamine N-acetyltransferase 1An arylamine N-acetyltransferase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P18440]Homo sapiens (human)

Compounds (1)

CompoundDefinitionClassesRoles
(z)-5-(2'-hydroxybenzylidene)-2-thioxothiazolidin-4-one(Z)-5-(2'-hydroxybenzylidene)-2-thioxothiazolidin-4-one: arylamine N-acetyltransferase 1inhibitor; structure in first source