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Pharmacogenomics of the cytochrome P450 2C family: impacts of amino acid variations on drug metabolism

机译:细胞色素P450 2C系列的药物替补:氨基酸变异对药物代谢的影响

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摘要

Pharmacogenomics investigates DNA and RNA variations in the human genome related to drug responses. Cytochrome P450 (CYP) is a supergene family of drug-metabolizing enzymes responsible for the metabolism of approximately 90% of human drugs. Among the major CYP isoforms, the CYP2C subfamily is of clinical significance because it metabolizes approximately 20% of clinically administrated drugs and represents several variant alleles leading to adverse drug reactions or altering drug efficacy. Here, we review recent progress on understanding the interindividual variability of the CYP2C members and the functional and clinical impact on drug metabolism. We summarize current advances in the molecular modeling of CYP2C polymorphisms and discuss the structural bases and molecular mechanisms of amino acid variants of CYP2C members that affect drug metabolism.
机译:药癌组学研究了与药物反应有关的人类基因组的DNA和RNA变化。 细胞色素P450(CYP)是一种超级基础类药物代谢酶,其负责约90%的人类药物的代谢。 在主要CYP同种型中,CYP2C亚家族具有临床意义,因为它代谢了大约20%的临床施用药物,并且代表了几个变异等位基因,导致药物不良反应或改变药物功效。 在这里,我们审查了最近了解CYP2C成员的联系变异性以及对药物代谢的功能和临床影响的进展。 我们总结了CYP2C多态性的分子模拟中的电流进展,并讨论了影响药物代谢的CYP2C成员氨基酸变体的结构基础和分子机制。

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  • 来源
    《Drug discovery today》 |2017年第2期|共11页
  • 作者单位

    West Univ Timisoara Dept Biol &

    Chem 16 Pestalozzi Timisoara 300115 Romania;

    Univ Paris Diderot Sorbonne Paris Cite Inserm UMR S 973 Mol Therapeut In Sil 39 Rue Helene;

    West Univ Timisoara Dept Biol &

    Chem 16 Pestalozzi Timisoara 300115 Romania;

    West Univ Timisoara Teacher Training Dept Blvd V Parvan Timisoara 300223 Romania;

    Ctr Univ St Peres INSERM UMR S1147 45 Rue St Peres F-75006 Paris France;

    Univ Paris Diderot Sorbonne Paris Cite Inserm UMR S 973 Mol Therapeut In Sil 39 Rue Helene;

    Univ Paris Diderot Sorbonne Paris Cite Inserm UMR S 973 Mol Therapeut In Sil 39 Rue Helene;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;
  • 关键词

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