Published : 2016-12-11

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

Grażyna Kubiak-Tomaszewska

Jan Pachecka

Jacek Łukaszkiewicz

Piotr Tomaszewski

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

Keywords:

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



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

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Editorial Team
Stefana Banacha 1
02-097 Warsaw, Poland
biuletynfarmacji@wum.edu.pl
Publisher:
Medical University of Warsaw
ul. Żwirki i Wigury 61
02-091 Warszawa

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