Related Experiment Video

Updated: Mar 1, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
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Differential Regulation of CYP3A4 and CYP3A5 and its Implication in Drug Discovery

Ogheneochukome Lolodi1, Yue-Ming Wang1, William C Wright1,2

  • 1Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, TN 38105, USA.

Current Drug Metabolism
|June 1, 2017
PubMed
Abstract

Insights

Cancer cells resist drugs by upregulating xenobiotic response systems, including pregnane X receptor (PXR) and CYP3A enzymes. Targeting these pathways offers potential for novel cancer therapies.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Cancer cells develop drug resistance through mechanisms like increased xenobiotic efflux and metabolic inactivation.
  • Xenobiotic metabolism involves Phase I and Phase II enzymes converting compounds into excretable forms.

Purpose of the Study:

  • To review the role of P450 (CYP) 3A enzymes, specifically CYP3A4 and CYP3A5, in cancer drug resistance.
  • To investigate the upregulation of xenobiotic response system components in cancer.

Main Methods:

  • A structured literature search was conducted focusing on P450 (CYP) 3A, CYP3A4, and CYP3A5.
  • Analysis of recent reports on the upregulation of xenobiotic response system components in diseases, including cancer.

Main Results:

  • Pregnane X receptor (PXR), CYP3A4, and CYP3A5 are upregulated in various cancers.
  • CYP3A enzymes are transcriptionally activated by PXR and its ligands.

Conclusions:

  • Aberrant expression of PXR and CYP3A enzymes in cancer is an active area of research.
  • Understanding these pathways may lead to the development of novel drugs targeting cancer resistance mechanisms.
Keywords:
CYP3A4CYP3A5Cancercytochrome P450drug discoverydrug resistancedrug-drug interactions

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