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Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation
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Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation

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Pharmacological Applications of Nrf2 Inhibitors as Potential Antineoplastic Drugs

Pelin Telkoparan-Akillilar1, Sibel Suzen2, Luciano Saso3

  • 1Department of Medical Biology, Faculty of Medicine, Yuksek Ihtisas University, 06520 Balgat, Ankara, Turkey. pelinta@yiu.edu.tr.

International Journal of Molecular Sciences
|April 27, 2019
PubMed

Insights

Nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) is a key controller of oxidative stress and a target for cancer therapy. This review discusses Nrf2 pathway modulation for anticancer treatments and its associated challenges.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Oxidative stress (OS) is implicated in numerous diseases, including cancer and neurodegenerative disorders.
  • The Nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) pathway is a critical cellular defense mechanism against OS.
  • Nrf2 pathway modulation is a promising strategy for antineoplastic treatments.

Purpose of the Study:

  • To review the modulation of the Nrf2 pathway in the context of cancer.
  • To discuss the anticancer activities associated with Nrf2 pathway activation.
  • To highlight the challenges in developing Nrf2-based anti-cancer therapies.

Main Methods:

  • Literature review of studies on Nrf2 pathway modulation and its role in cancer.
  • Analysis of research on Nrf2 activators as chemopreventive agents.
  • Discussion of findings regarding Nrf2 hyperactivation in cancer cell survival.

Main Results:

  • Nrf2 is a potent cytoprotective regulator against OS.
  • Nrf2 activators are explored for cancer chemoprevention, despite Nrf2 activation in various cancers.
  • Hyperactivation of Nrf2 promotes survival of both normal and malignant cells against OS, chemotherapy, and radiotherapy.

Conclusions:

  • Modulating the Nrf2 pathway presents a significant strategy for cancer treatment.
  • Understanding Nrf2's dual role in cancer is crucial for therapeutic development.
  • Further research is needed to overcome challenges in developing effective Nrf2-based anti-cancer drugs.
Keywords:
Nrf2 inhibitorsantineoplastic drugscancercancer chemoprevention and therapychemoresistance

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