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Arylamine N-acetyltransferases 3

Part 3 of 3
Published on October 1, 2007 Updated on July 28, 2016   19 min

A selection of talks on Pharmaceutical Sciences

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0:00
Arylamine N-acetyltransferases. Part 3 I'm Edith Sim, and I have been working on these enzymes for over 20 years.
0:10
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.
0:40
In order to explore this further, it was felt important to identify NAT1 specific inhibitors.
0:51
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.
1:11
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.

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