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Bioorg Med Chem Lett. 2004 Aug 16;14(16):4217-20.

Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.

Author information

1
College of Pharmacy, University of Michigan, 428 Church Street, Ann Arbor, MI 48109, USA.

Abstract

Inhibitors of phenylethanolamine N-methyltransferase [PNMT, the enzyme that catalyzes the final step in the biosynthesis of epinephrine (Epi)] may be of use in determining the role of Epi in the central nervous system. Here we demonstrate that a routinely used assay for screening PNMT inhibitors is not appropriate for those inhibitors having K(i) values less than 1 microM. A revised assay has been developed that shows some inhibitors bind two orders of magnitude more tightly than previously reported.

PMID:
15261273
DOI:
10.1016/j.bmcl.2004.06.009
[Indexed for MEDLINE]

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