title: Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.
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.
authors.affiliation: College of Pharmacy, University of Michigan, 428 Church Street, Ann Arbor, MI 48109, USA.
authors.forename: Qian
authors.initials: Q
authors.lastname: Wu
authors.forename: Kevin R
authors.initials: KR
authors.lastname: Criscione
authors.forename: Gary L
authors.initials: GL
authors.lastname: Grunewald
authors.forename: Michael J
authors.initials: MJ
authors.lastname: McLeish
mesh_terms: D004791:Enzyme Inhibitors / Q000494:pharmacology; D007700:Kinetics; D010625:Phenylethanolamine N-Methyltransferase / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D010625:Phenylethanolamine N-Methyltransferase