MECHANISMS OF RECEPTOR-DEPENDENT REGULATION OF BILE ACID AND XENOBIOTIC METABOLISM. THE ROLE OF CYP3A4 EXPRESSION IN THE SAFETY AND EFFECTIVENESS OF PHARMACOTHERAPY

Authors

  • Grażyna Kubiak-Tomaszewska Zakład Biochemii i Chemii Klinicznej, Wydział Farmaceutyczny z Oddziałem Medycyny Laboratoryjnej, Warszawski Uniwersytet Medyczny, ul. Banacha 1, 02-097 Warszawa
  • Jan Pachecka Wydział Ekologii, Wyższa Szkoła Ekologii i Zarządzania w Warszawie, ul. Olszewska 12, 00-792 Warszawa; Wydział Ekologii, Wyższa Szkoła Ekologii i Zarządzania w Warszawie, ul. Olszewska 12, 00-792 Warszawa
  • Jacek Łukaszkiewicz Zakład Biochemii i Chemii Klinicznej, Wydział Farmaceutyczny z Oddziałem Medycyny Laboratoryjnej, Warszawski Uniwersytet Medyczny, ul. Banacha 1, 02-097 Warszawa
  • Piotr Tomaszewski Zakład Biochemii i Chemii Klinicznej, Wydział Farmaceutyczny z Oddziałem Medycyny Laboratoryjnej, Warszawski Uniwersytet Medyczny, ul. Banacha 1, 02-097 Warszawa

DOI:

https://doi.org/10.56782/pps.118

Keywords:

CYP3A4, expression, regulation, nuclear receptors, PXR, FXR, xenobiotic biotransformation, drug metabolism, bile acids, pharmacotherapy

Abstract

The isoenzyme CYP3A4 is an important monooxygenase responsible for the metabolism of a large variety of endogenous and exogenous compounds (xenobiotics), including more than 50% of known drugs. The highest activity of CYP3A4 in human was found in hepatocytes and enterocytes. CYP3A4 gene expression is regulated by diverse exogenous and endogenous factors, including bile acids and several drugs, acting via nuclear receptors, such as, for example, PXR or FXR. Understanding the mechanisms of CYP3A4 gene expression is essential for ensuring the safety and effectiveness of pharmacotherapy.

KEYWORDS: CYP3A4, expression, regulation, nuclear receptors, PXR, FXR, xenobiotic biotransformation, drug metabolism, bile acids, pharmacotherapy

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Author Biography

  • Grażyna Kubiak-Tomaszewska, Zakład Biochemii i Chemii Klinicznej, Wydział Farmaceutyczny z Oddziałem Medycyny Laboratoryjnej, Warszawski Uniwersytet Medyczny, ul. Banacha 1, 02-097 Warszawa

    autorka korespondująca, tel: +48 22 5720764

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2016-12-11

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How to Cite

MECHANISMS OF RECEPTOR-DEPENDENT REGULATION OF BILE ACID AND XENOBIOTIC METABOLISM. THE ROLE OF CYP3A4 EXPRESSION IN THE SAFETY AND EFFECTIVENESS OF PHARMACOTHERAPY. (2016). Prospects in Pharmaceutical Sciences, 14(9), 57-63. https://doi.org/10.56782/pps.118

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