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Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
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NRF2 Modulators of Plant Origin and Their Ability to Overcome Multidrug Resistance in Cancers

Piotr Wadowski1,2, Michał Juszczak1, Katarzyna Woźniak1

  • 1Department of Molecular Genetics, Faculty of Biology and Environmental Protection, University of Lodz, Pomorska 141/143, 90-236 Lodz, Poland.

International Journal of Molecular Sciences
|November 9, 2024
PubMed

Insights

Plant-derived compounds that inhibit the NRF2 pathway can help overcome multidrug resistance (MDR) in cancer. This approach targets a key factor in chemotherapy ineffectiveness, offering new therapeutic strategies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Cancer remains a leading cause of death globally, with chemotherapy often failing due to multidrug resistance (MDR).
  • The transcription factor NRF2 (Nuclear factor erythroid 2-related factor 2) plays a dual role: protecting normal cells from oxidative stress but promoting MDR in cancer cells.
  • Hyperactivation of NRF2 in cancer cells leads to the upregulation of genes (e.g., HO-1, NQO1, MRP1, MRP2, GST) that confer resistance to chemotherapy.

Purpose of the Study:

  • To review the current knowledge on plant-derived NRF2 inhibitors.
  • To explore the potential of NRF2 inhibition as a strategy to overcome MDR in cancer treatment.

Main Methods:

  • Literature review of studies investigating plant compounds targeting the NRF2 pathway.
  • Analysis of research on the role of NRF2 in MDR and the efficacy of its inhibitors.

Main Results:

  • NRF2 is a critical factor in the development of MDR, significantly limiting chemotherapy effectiveness.
  • Numerous plant compounds have been identified as NRF2 modulators, with many acting as inhibitors.
  • Inhibition of NRF2 by plant-derived compounds shows promise in reversing MDR and enhancing chemotherapy efficacy.

Conclusions:

  • NRF2 inhibition is a promising strategy for overcoming chemotherapy resistance in cancer.
  • Plant-derived NRF2 inhibitors represent a valuable resource for developing novel anticancer therapies.
  • Targeting NRF2 could be a key component in future cancer treatment regimens to improve patient outcomes.
Keywords:
NRF2 activatorsNRF2 inhibitorsalkaloidscancermultidrug resistancepolyphenols

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