Human Arylamine N-acetyltransferase 1: From Drug Metabolism to Drug Target

Human arylamine N-acetyltransferase 1 (NAT1) is a phase II xenobiotic-metabolizing enzyme (XME) involved in the biotransformation of many aromatic amines and heterocyclic amines. This XME is known to play important roles in both the detoxication and/or bioactivation of numerous drugs and carcinogens. NAT1 is a polymorphic enzyme with a large tissue distribution. NAT1 polymorphisms and activity have been extensively studied because of its potential role in the biotransformation of important carcinogens. Several studies suggest that NAT1 may have a role in breast cancer progression. Indeed, this XME has been shown to affect the growth and drug resistance of breast cancer cells and appears as a marker in human estrogen receptor–positive breast cancer. In addition, it has been shown that this enzyme is inhibited in vivo by cancer drugs such as cisplatin or tamoxifen. Recent published data suggest that NAT1 could be targeted for breast cancer therapy. Here, we provide an overview on the putative role of NAT1 in cancer and on its useful role as a drug target.