Xanthates: Metabolism by Flavoprotein-Containing Monooxygenases and Antimycobacterial Activity
نویسندگان
چکیده
منابع مشابه
Flavin Containing Monooxygenases and Metabolism of Xenobiotics
Bu derlemede flavin-içeren monooksijenazların (FMO) farmakolojik ve toksikolojik önemi ile ilgili güncel bilgiler özetlenmiştir. FMO’lar nükleofilik hetereatom içeren ksenobiyotiklerin ve ilaçların oksidasyonuna katılan mikrozomal bir enzim ailesidir. FMO’ların ilaç metabolizmasındaki etkinlikleri ve hastalıklarla olan ilişkileri, daha fazla araştırılması gereken alanlardır. FMO’lar üzerine yap...
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Mammalian flavin-containing monooxygenases, which are difficult to obtain and study, play a major role in detoxifying various xenobiotics. To provide alternative biocatalytic tools to generate flavin-containing monooxygenases (FMO)-derived drug metabolites, a collection of microbial flavoprotein monooxygenases, sequence-related to human FMOs, was tested for their ability to oxidize a set of xen...
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The N-hydroxylating flavoprotein monooxygenases are siderophore biosynthetic enzymes that catalyze the hydroxylation of the sidechain amino-group of ornithine or lysine or the primary amino-group of putrescine. This hydroxylated product is subsequently formylated or acylated and incorporated into the siderophore. Importantly, the modified amino-group is a hydroxamate and serves as an iron chela...
متن کاملGenetic Variants of Flavin-containing Monooxygenases: Consequences for Drug Metabolism
The metabolism of the anti-tubercular drug, thiacetazone (TAZ) by human FMOs in vitro and the disposition of TAZ in vivo in mice were studied. Reverse phase chromatography confirmed TAZ to be a substrate for human FMO1, FMO2.1 and FMO3 with the formation of TAZ-sulphinic acid and TAZ-carbodiimide via a TAZsulphenic acid intermediate. The products are the same as those formed by the Mycobacteriu...
متن کاملMetabolism of ketoconazole and deacetylated ketoconazole by rat hepatic microsomes and flavin-containing monooxygenases.
Ketoconazole (KT) has been reported to cause hepatotoxicity, which is probably not mediated through an immunoallergic mechanism. Although KT is extensively metabolized by hepatic microsomal enzymes, the nature, route of formation, and toxicity of suspected metabolites are largely unknown. Recent reports indicate that N-deacetyl ketoconazole (DAK) is a major initial metabolite in mice, which, li...
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ژورنال
عنوان ژورنال: Drug Metabolism and Disposition
سال: 2018
ISSN: 0090-9556,1521-009X
DOI: 10.1124/dmd.118.081984