Article
Mechanism-based inhibition of the melatonin rhythm enzyme: pharmacologic exploitation of active site functional plasticity.
Proceedings of the National Academy of Sciences of the United States of America - 26 Oct 1999
Khalil E M, De Angelis J, Ishii M, Cole P A
Abstract excerpt
Serotonin N-acetyltransferase is the enzyme responsible for the diurnal rhythm of melatonin production in the pineal gland of animals and humans. Inhibitors of this enzyme active in cell culture have not been reported previously. The compound N-bromoacetyltryptamine was shown to be a potent inhibitor of this enzyme in vitro and in a pineal cell culture assay (IC(50) approximately 500 nM). The mechanism of...
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