Arylamine N-acetyltransferases 3

Published on October 1, 2007 Updated on July 28, 2016   19 min

A selection of talks on Metabolism & Nutrition

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Arylamine N-acetyltransferases. Part 3 I'm Edith Sim, and I have been working on these enzymes for over 20 years.
So human NAT1, to recap, is widespread in tissue distribution, shows genetic polymorphism, N-acetylates p-aminobenzoic acid, and N-acetylates p-abaglu a folate catabolite. It hydrolyses acetylCoA in the presence of folate. It's clearly expressed in early development. It's over-expressed in ER positive breast cancer. And it's linked to folate and acetylCoA homeostasis.
In order to explore this further, it was felt important to identify NAT1 specific inhibitors.
This was done, again, you've seen this slide before, but just to emphasize, this was done to allow a library of over 5,000 compounds to be screened with recombinant specific enzymes including human NAT1.
What came out of this was a specific NAT1 inhibitor, identified as naphthoquinone, which when it binds to human NAT1 changes color from red to blue. This is important because if NAT1 is a biomarker for breast cancer, then having something which would specifically detect it is particularly important.