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Synthetic Na+/K+ exchangers promote apoptosis by disturbing cellular cation homeostasis

Sang-Hyun Park1,2, Inhong Hwang3,2, Daniel A McNaughton4,2

  • 1Department of Chemistry, Yonsei University, Seoul 03722, Republic of Korea.

Chem
|January 19, 2024
PubMed

Insights

New synthetic ion-pair receptors efficiently exchange sodium (Na+) and potassium (K+) ions. This ion exchange in cancer cells induces apoptosis by disrupting cellular cation homeostasis and ER stress.

Area of Science:

  • Chemical Biology
  • Molecular Biology
  • Biomedical Applications

Background:

  • Artificial cation ionophores are crucial for research and medicine.
  • Understanding ionophore mechanisms and their link to cell death is limited.

Purpose of the Study:

  • To investigate the function of hemispherand-strapped calix[4]pyrrole-based ion-pair receptors.
  • To elucidate the mechanism by which these receptors induce cancer cell apoptosis.

Main Methods:

  • Utilized liposomal models to study ion-pair receptor activity.
  • Investigated Na+/K+ exchange in cancer cells.
  • Performed mechanistic studies on endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and mitochondrial apoptosis.

Main Results:

  • Three hemispherand-strapped calix[4]pyrrole derivatives function as efficient Na+/K+ exchangers.
  • These receptors promote Na+ influx and K+ efflux in cancer cells, inducing apoptosis.
  • The mechanism involves perturbation of intracellular cation homeostasis, leading to ER stress, ROS generation, and mitochondria-mediated apoptosis.

Conclusions:

  • Synthetic receptors that disrupt cellular cation homeostasis offer potential as novel small molecules with apoptotic activity.
  • Hemispherand-strapped calix[4]pyrrole-based receptors demonstrate a promising approach for inducing cancer cell death.

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