Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.
Article Details
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Wu Q, Criscione KR, Grunewald GL, McLeish MJ
Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.
Bioorg Med Chem Lett. 2004 Aug 16;14(16):4217-20.
- PubMed ID
- 15261273 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 1,2,3,4-Tetrahydro-Isoquinoline-7-Sulfonic Acid Amide Phenylethanolamine N-methyltransferase Ki (nM) 280 N/A N/A Details 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline Phenylethanolamine N-methyltransferase Ki (nM) 3.1 N/A N/A Details 8,9-Dichloro-2,3,4,5-Tetrahydro-1h-Benzo[C]Azepine Phenylethanolamine N-methyltransferase Ki (nM) 10 N/A N/A Details