顺式和反式5-氨甲基-3-(4-甲氧基苯基)二氢呋喃-2(3H)-酮对单胺氧化酶B的失活作用

Inactivation of monoamine oxidase B by cis- and trans-5-aminomethyl-3-(4-methoxyphenyl)dihydrofuran-2(3H)-ones.

作者信息

Lu X, Silverman R B

机构信息

Department of Chemistry, Northwestern University, Evanston, IL 60208-3113, USA.

出版信息

Bioorg Med Chem. 1998 Oct;6(10):1851-6. doi: 10.1016/s0968-0896(98)00116-3.

DOI:10.1016/s0968-0896(98)00116-3

PMID:9839014

Abstract

Monoamine oxidase B was previously shown to be inactivated by cis- (3) and trans-5-(aminomethyl)-3-(4-methoxyphenyl)dihydrofuran-2(3H)-one hydrochloride (4) in a time-dependent manner (Ding, Z.; Silverman, R. B. J. Med. Chem. 1992, 35, 885) and to catalyze its oxidative decarboxylation (Silverman, R. B.; Zhou, J.J.P.; Ding, C. Z.; Lu, X. J. Am. Chem. Soc. 1995, 117, 12895). By [14C]-labeling of the aryl methoxyl groups of these two inactivators, it is shown that this is not a mechanism-based inactivation and that multiple enzyme residues are labeled.

摘要

先前已表明，单胺氧化酶B会被顺式-（3）和反式-5-（氨甲基）-3-（4-甲氧基苯基）二氢呋喃-2（3H）-酮盐酸盐（4）以时间依赖性方式失活（丁，Z.；西尔弗曼，R. B.《药物化学杂志》1992年，35卷，885页），并且它能催化其氧化脱羧反应（西尔弗曼，R. B.；周，J. J. P.；丁，C. Z.；卢，X.《美国化学会志》1995年，117卷，12895页）。通过对这两种失活剂的芳基甲氧基进行[14C]标记，结果表明这不是基于机制的失活，并且多个酶残基被标记。