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Research ArticleMinireview

Transcriptional Regulation of CYP2D6 Expression

Xian Pan, Miaoran Ning and Hyunyoung Jeong
Drug Metabolism and Disposition January 2017, 45 (1) 42-48; DOI: https://doi.org/10.1124/dmd.116.072249
Xian Pan
Department of Biopharmaceutical Sciences (X.P., M.N., H.J.), and Department of Pharmacy Practice (H.J.), College of Pharmacy, University of Illinois at Chicago, Chicago, Illinois
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Miaoran Ning
Department of Biopharmaceutical Sciences (X.P., M.N., H.J.), and Department of Pharmacy Practice (H.J.), College of Pharmacy, University of Illinois at Chicago, Chicago, Illinois
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Hyunyoung Jeong
Department of Biopharmaceutical Sciences (X.P., M.N., H.J.), and Department of Pharmacy Practice (H.J.), College of Pharmacy, University of Illinois at Chicago, Chicago, Illinois
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Abstract

CYP2D6-mediated drug metabolism exhibits large interindividual variability. Although genetic variations in the CYP2D6 gene are well known contributors to the variability, the sources of CYP2D6 variability in individuals of the same genotype remain unexplained. Accumulating data indicate that transcriptional regulation of CYP2D6 may account for part of CYP2D6 variability. Yet, our understanding of factors governing transcriptional regulation of CYP2D6 is limited. Recently, mechanistic studies of increased CYP2D6-mediated drug metabolism in pregnancy revealed two transcription factors, small heterodimer partner (SHP) and Krüppel-like factor 9, as a transcriptional repressor and an activator, respectively, of CYP2D6. Chemicals that increase SHP expression (e.g., retinoids and activators of farnesoid X receptor) were shown to downregulate CYP2D6 expression in the humanized mice as well as in human hepatocytes. This review summarizes the series of studies on the transcriptional regulation of CYP2D6 expression, potentially providing a basis to better understand the large interindividual variability in CYP2D6-mediated drug metabolism.

Footnotes

    • Received July 5, 2016.
    • Accepted September 29, 2016.
  • This work was supported by the National Institutes of Health [Grants R01HD065532 and R01GM112746]. M.N. is a recipient of a Graduate Student Fellowship Award from the American Association of Pharmaceutical Scientists Foundation.

  • dx.doi.org/10.1124/dmd.116.072249.

  • Copyright © 2016 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 45 (1)
Drug Metabolism and Disposition
Vol. 45, Issue 1
1 Jan 2017
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Research ArticleMinireview

CYP2D6 Transcriptional Regulation

Xian Pan, Miaoran Ning and Hyunyoung Jeong
Drug Metabolism and Disposition January 1, 2017, 45 (1) 42-48; DOI: https://doi.org/10.1124/dmd.116.072249

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Research ArticleMinireview

CYP2D6 Transcriptional Regulation

Xian Pan, Miaoran Ning and Hyunyoung Jeong
Drug Metabolism and Disposition January 1, 2017, 45 (1) 42-48; DOI: https://doi.org/10.1124/dmd.116.072249
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  • Article
    • Abstract
    • Introduction
    • Genetic Polymorphisms of CYP2D6 that Modulate CYP2D6 Expression
    • Transcription Factors Involved in the Regulation of Basal CYP2D6 Expression
    • Transcriptional Regulation of CYP2D6 during Pregnancy
    • Modulators of CYP2D6 Transcription
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