Pharmacogenetics, Regulation and Structural Properties of the Drugmetabolizing Enzymes Arylamine N-acetyltransferases
Xenobiotic-metabolizing enzymes (XME) are responsible for the biotransformation of a vast range of compounds. Arylamine N-acetyltransferases (NAT) are XME responsible for the acetylation of many arylamine and heterocyclic amines. They therefore, play an important role in the detoxification and activation of numerous drugs and carcinogens. Two closely related isoforms (NAT1 and NAT2) have been described in humans. NAT2 is present mainly in the liver and gut whereas NAT1 is found in a wide range of tissues. Interindividual variations in NAT genes have been shown to be a potential source of pharmacological and / or pathological susceptibility. In addition, there is now evidence that non genetic factors, such as substrate-dependent inhibition or redox conditions, may also contribute to overall NAT1 activity. This mini-review summarizes current knowledge on human NATs. Recent aspects of NAT gene expression, regulation and structural properties are discussed.
Keywords: arylamine n-acetyltransferases; catalytic activity; expression; phenotypes; polymorphism; xenobiotic-metabolizing enzymes
Document Type: Review Article
Affiliations: CNRS-UMR7000, Faculte de Medecine Pitie-Salpetriere, 105 bd de l'Hopital, 75013 Paris, France.
Publication date: 01 December 2004
- Current Pharmacogenomics provides comprehensive overviews of all current research on pharmacogenomics and pharmacogenetics. All areas of the field from pre-clinical to clinical research are covered, including related areas such as genomics, proteomics, target discovery, bioinformatics and novel diagnostics. This international journal is peer-reviewed and publishes both mini- and full review articles.
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