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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.
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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.
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In order
to explore this further,
it was felt important
to identify
NAT1 specific inhibitors.
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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.
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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.
