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  • Regulation of drug-metabolizing cytochromes P450 (CYPs) occurs via multiple mechanisms. A pivotal means of CYP regulation is transcriptional control, which influences the expression and the amount of the enzyme. Many xenobiotics, including therapeutically used drugs, upregulate (induce) the expression of CYPs by transcriptional mechanisms. Xenobiotic-mediated induction of CYPs results in altered intermediary metabolism as well as the metabolism of drugs and it is, hence, a serious cause of drug-drug interactions. The current chapter summarizes our knowledge on the transcriptional regulation of drug-inducible CYPs comprising CYP1A1, CYP1A2, CYP1B1, CYP2A6, CYP2B6, CYP2Cs, and CYP3A4 genes. The role of pregnane X receptor, constitutive androstane receptor, aryl hydrocarbon receptor, steroid receptors (glucocorticoid receptor, estrogen receptor), nuclear receptors (vitamin D receptor, retinoic X receptor, liver X receptor) and transcriptional factors (HNF-4, C/EBP, SMRT, etc.) is explained.
  • Regulation of drug-metabolizing cytochromes P450 (CYPs) occurs via multiple mechanisms. A pivotal means of CYP regulation is transcriptional control, which influences the expression and the amount of the enzyme. Many xenobiotics, including therapeutically used drugs, upregulate (induce) the expression of CYPs by transcriptional mechanisms. Xenobiotic-mediated induction of CYPs results in altered intermediary metabolism as well as the metabolism of drugs and it is, hence, a serious cause of drug-drug interactions. The current chapter summarizes our knowledge on the transcriptional regulation of drug-inducible CYPs comprising CYP1A1, CYP1A2, CYP1B1, CYP2A6, CYP2B6, CYP2Cs, and CYP3A4 genes. The role of pregnane X receptor, constitutive androstane receptor, aryl hydrocarbon receptor, steroid receptors (glucocorticoid receptor, estrogen receptor), nuclear receptors (vitamin D receptor, retinoic X receptor, liver X receptor) and transcriptional factors (HNF-4, C/EBP, SMRT, etc.) is explained. (en)
Title
  • Transcriptional Regulation of Human Drug-Metabolizing Cytochrome P450 Enzymes
  • Transcriptional Regulation of Human Drug-Metabolizing Cytochrome P450 Enzymes (en)
skos:prefLabel
  • Transcriptional Regulation of Human Drug-Metabolizing Cytochrome P450 Enzymes
  • Transcriptional Regulation of Human Drug-Metabolizing Cytochrome P450 Enzymes (en)
skos:notation
  • RIV/61989592:15310/12:33142726!RIV13-GA0-15310___
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  • P(GAP304/10/0149), P(GAP503/10/0579)
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  • 174854
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  • RIV/61989592:15310/12:33142726
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  • cytochrome P450, nuclear receptor, xenoreceptor, steroid receptor, induction, drug, metabolism (en)
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  • [557FE20BB47C]
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  • Weinheim
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  • Neuveden
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  • Metabolism of Drugs and Other Xenobiotics
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  • Dvořák, Zdeněk
number of pages
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  • Wiley-VCH Verlag
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  • 978-3-527-32903-8
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  • 15310
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