Arylamine N-acetyltransferase

Function

Arylamine N-acetyltransferase (NAT) catalyzes the transfer of an acetyl group from acetyl-CoA to an arylamine. Human NAT have 2 polymorphs with different substrate specificities. NAT1 acetylates p-aminisalycilates while NAT2 acetylates hydralazine.

Disease

Human NAT1 is overexpressed in some kinds of breast cancer.

Relevance

Acetylation is a major route of biotransformation for many arylamines and hydrazine drugs and known carcinogens like cigarette smoke. The levels of NAT in the body has important consequences with regard to an individual’s susceptibility to certain drug-induced toxicities and cancer.

Structural highlights

NAT acetylates using a catalytic Cys-His-Asp triad.