Flavin Containing Monooxygenases and Metabolism of Xenobiotics

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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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Genetic 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...

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Metabolism 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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Short Communication Metabolism 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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Human kidney flavin-containing monooxygenases and their potential roles in cysteine s-conjugate metabolism and nephrotoxicity.

The potential roles of human hepatic and renal flavin-containing monooxygenases (FMOs) in the metabolism of the cysteine S-conjugates S-allyl cysteine (SAC) and S-(1,2-dichlorovinyl)-L-cysteine (DCVC) were investigated. Incubations of human cDNA-expressed FMO1, FMO3, FMO4, and FMO5 with SAC resulted in detection of SAC sulfoxide, with FMO3 exhibiting approximately 3-, 4-, and 10-fold higher act...

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ژورنال

عنوان ژورنال: Turkish Journal of Pharmaceutical Sciences

سال: 2017

ISSN: 1304-530X,2148-6247

DOI: 10.4274/tjps.30592