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Updated: Dec 28, 2025

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
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Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms

Published on: December 9, 2015

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Emerging roles for UDP-glucuronosyltransferases in drug resistance and cancer progression

Eric P Allain1,2, Michèle Rouleau1,2, Eric Lévesque1,3

  • 1Pharmacogenomics Laboratory, Centre Hospitalier Universitaire (CHU) de Québec Research Center-Laval University, Québec, QC, Canada.

British Journal of Cancer
|February 13, 2020
PubMed

Insights

UDP-glucuronosyltransferase enzymes (UGTs) are crucial in cancer therapy, impacting drug resistance and progression. Understanding UGTs offers new strategies for cancer treatment and improved drug efficacy.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Oncology

Background:

  • UDP-glucuronosyltransferase enzymes (UGTs) are known for metabolizing drugs, affecting their efficacy and elimination.
  • UGTs play a role in drug resistance and response modulation across various cancer types.
  • Emerging evidence links UGT dysregulation to cancer progression, independent of drug treatment.

Purpose of the Study:

  • To review the dual roles of UGTs in cancer, encompassing drug resistance and intrinsic cancer progression.
  • To explore the impact of altered UGT activity on tumor biology and endogenous metabolite levels.
  • To highlight the potential of UGTs as biomarkers and therapeutic targets in oncology.

Main Methods:

  • Literature review of clinical observations and experimental evidence.
  • Analysis of studies investigating UGT expression, activity, and their association with cancer outcomes.
  • Synthesis of data on UGTs' influence on drug metabolism and endogenous signaling pathways.

Main Results:

  • UGTs significantly modulate the response to anti-cancer drugs, contributing to resistance.
  • Dysregulated UGTs are implicated in the progression of several cancers, potentially via altered endogenous metabolite inactivation.
  • Altered UGT activity may impact tumor biology through perturbed steroid and lipid metabolism, activating oncogenic pathways.

Conclusions:

  • UGTs exhibit dual roles in cancer, influencing both drug resistance and cancer progression.
  • Targeting UGTs or utilizing UGT pharmacogenomics may offer novel prognostic and predictive biomarkers.
  • Developing strategies to modulate UGT activity holds promise for enhancing anti-cancer drug efficacy.

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