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Updated: Mar 28, 2026
Author Spotlight: Exploring the Role of Ion Channels in Cancer: Characterization and Potential Treatment Approaches
Published on: June 16, 2023
Pharmacological targeting of ion channels for cancer therapy: In vivo evidences
Luigi Leanza1, Antonella Managò1, Mario Zoratti2
1Department of Biology, University of Padua, Padua, Italy.
Abstract:
Since the discovery of the participation of various ion channels in the regulation of cell proliferation and programmed cell death two decades ago, the field exploring ion channel function in relation to cancer has undergone rapid development. Although the mechanisms accounting for the impact of ion channel modulators on cancer growth have not been fully clarified in all cases, numerous in vivo experiments targeting diverse ion channels in various cancer models illustrate the great potentiality of this approach and promote ion channels to the class of oncological targets. In the present review we give an updated overview of the field and critically discuss the promising results obtained in pre-clinical models using specific pharmacological modulators of calcium, sodium, potassium and anion-permeable ion channels, whose expression is often altered in tumor cells and tissues. The most, especially critical issues are specificity of action and side-effects. Interestingly, some of the most potent drugs are natural products, and several of the active compounds are already used in the clinic for other purposes. In these latter cases involving drug repositioning we may expect a faster progression from preclinical to clinical studies. This article is part of a Special Issue entitled: Calcium and Cell Fate. Guest Editors: Jacques Haiech, Claus Heizmann, Joachim Krebs, Thierry Capiod and Olivier Mignen.
Insights
Ion channels regulate cell death and proliferation, emerging as key cancer targets. Research shows targeting these channels, including calcium, sodium, and potassium, holds significant therapeutic potential for cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Biophysics
Background:
- Ion channels play crucial roles in cell proliferation and programmed cell death.
- Their dysregulation is frequently observed in tumor cells and tissues, highlighting their oncogenic potential.
- The field of ion channel research in cancer has rapidly advanced over the past two decades.
Purpose of the Study:
- To provide an updated overview of ion channel involvement in cancer.
- To critically discuss preclinical findings on ion channel modulators in cancer models.
- To highlight challenges and opportunities in targeting ion channels for cancer therapy.
Main Methods:
- Review of preclinical studies utilizing specific pharmacological modulators of calcium, sodium, potassium, and anion-permeable ion channels.
- Analysis of in vivo experiments in various cancer models.
- Discussion of drug repositioning strategies for ion channel modulators.
Main Results:
- Numerous ion channels (calcium, sodium, potassium, anion-permeable) are implicated in cancer progression.
- Pharmacological modulation of these channels shows promise in preclinical cancer models.
- Natural products and repositioned drugs are among the potent therapeutic agents identified.
Conclusions:
- Ion channels represent promising oncological targets with significant therapeutic potential.
- Further research is needed to clarify mechanisms and address specificity and side-effect issues.
- Drug repositioning offers a faster pathway for clinical translation of ion channel-targeted therapies.
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