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Updated: Jun 2, 2026

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
Published on: September 20, 2018
Epigenetic regulation of drug processing genes
Curtis D Klaassen1, Hong Lu, Julia Yue Cui
1Department of Pharmacology, Toxicology and Therapeutics, University of Kansas Medical Center, Kansas City, Kansas 66160, USA. cklaasse@kumc.edu
Epigenetic mechanisms like DNA methylation regulate drug processing genes (DPGs) and nuclear receptors. This regulation impacts tissue-specific expression, development, and cancer, crucial for understanding xenobiotic metabolism.
Area of Science:
- Pharmacology and Toxicology
- Molecular Biology
- Epigenetics
Background:
- Drug processing genes (DPGs) control xenobiotic absorption, distribution, metabolism, and excretion.
- Nuclear receptors/transcription factors regulate DPG expression.
- Epigenetic mechanisms, including DNA methylation, histone modifications, and microRNAs, are increasingly recognized as regulators of DPGs and nuclear receptors.
Purpose of the Study:
- To summarize current knowledge on the epigenetic regulation of DPGs and nuclear receptors.
- To highlight the role of epigenetics in tissue-specific gene expression.
- To examine epigenetic influences on gene expression during development and carcinogenesis.
Main Methods:
- Literature review and synthesis of existing research on epigenetic regulation of DPGs and nuclear receptors.
- Analysis of studies focusing on DNA methylation, histone modifications, and microRNA involvement.
- Examination of data related to tissue-specific expression, developmental changes, and cancer-related alterations.
Main Results:
- Epigenetic mechanisms significantly influence the expression of DPGs and nuclear receptors.
- These epigenetic modifications are critical for establishing and maintaining tissue-specific gene expression patterns.
- Alterations in epigenetic regulation of DPGs and nuclear receptors are implicated in developmental processes and the development of cancer.
Conclusions:
- Epigenetic regulation is a key determinant of DPG and nuclear receptor function.
- Understanding these epigenetic mechanisms is vital for comprehending xenobiotic metabolism, normal development, and disease pathogenesis, particularly cancer.
- Further research into epigenetic modifications offers potential therapeutic targets for diseases involving altered drug metabolism.
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