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

ABSTRACT: A number of artificial cation ionophores (or transporters) have been developed for basic research and biomedical applications. However, their mechanisms of action and the putative correlations between changes in intracellular cation concentrations and induced cell death remain poorly understood. Here, we show that three hemispherand-strapped calix[4]pyrrole-based ion-pair receptors act as efficient Na⁺/K⁺ exchangers in the presence of Cl^- in liposomal models and promote Na⁺ influx and K⁺ efflux (Na⁺/K⁺ exchange) in cancer cells to induce apoptosis. Mechanistic studies reveal that these cation exchangers induce endoplasmic reticulum (ER) stress in cancer cells by perturbing intracellular cation homeostasis, promote

SUBMITTER: Park SH 

PROVIDER: S-EPMC10795848 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature