Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.
Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.
复制标题
苯乙醇胺 N-甲基转移酶抑制：动力学数据的重新评估。
DOI：
10.1016/j.bmcl.2004.06.009
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发表时间：
2004
期刊：
影响因子：
--
通讯作者：
McLeish,MichaelJ
中科院分区：
文献类型：
--
作者：
Wu,Qian;Criscione,KevinR;Grunewald,GaryL;McLeish,MichaelJ
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 Kivalues less than 1μM. A revised assay has been developed that shows some inhibitors bind two orders of magnitude more tightly than previously reported.
