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黃素單氧化酶在藥物代謝和新藥研發(fā)中的作用

發(fā)布時(shí)間:2018-06-06 23:53

  本文選題:黃素單氧化酶 + 細(xì)胞色素P; 參考:《藥學(xué)學(xué)報(bào)》2017年10期


【摘要】:黃素單氧化酶(flavin-containing monooxygenases,FMOs)是僅次于細(xì)胞色素P450(cytochrome P450,CYP450)的重要Ⅰ相代謝酶,可催化含氮、硫、磷、硒等親核雜原子的外源物及部分內(nèi)源物的氧化反應(yīng)。本文將介紹FMOs的生物學(xué)特征、催化機(jī)制、底物特異性、基因多態(tài)性,分析FMOs對(duì)藥物代謝的影響和個(gè)體差異以及與FMOs代謝相關(guān)的疾病,為尋找新的作用靶點(diǎn)和設(shè)計(jì)候選藥物提供理論參考。
[Abstract]:Flavin-containing monooxygenase (FMOs) is an important phase I metabolic enzyme, which can catalyze the oxidation of nitrogen, sulfur, phosphorus, selenium and other nucleophilic heterophile exogenous and some endogenous compounds, which is second only to cytochrome P450(cytochrome P450 (CYP450). This paper will introduce the biological characteristics, catalytic mechanism, substrate specificity, gene polymorphism of FMOs, analyze the effects of FMOs on drug metabolism, individual differences and diseases related to FMOs metabolism. It provides a theoretical reference for finding new targets and designing candidate drugs.
【作者單位】: 中國(guó)醫(yī)學(xué)科學(xué)院北京協(xié)和醫(yī)學(xué)院藥物研究所藥物代謝室創(chuàng)新藥物非臨床藥代/藥效北京市重點(diǎn)實(shí)驗(yàn)室活性物質(zhì)發(fā)現(xiàn)與適藥化研究北京市重點(diǎn)實(shí)驗(yàn)室;
【基金】:十二五新藥創(chuàng)制重大專(zhuān)項(xiàng)資助項(xiàng)目(2012ZX09301002-001-007,2012ZX09301002-006,2012ZX09103-101-001)
【分類(lèi)號(hào)】:R96


本文編號(hào):1988678

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