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Synthetic Anion Transporters as Endoplasmic Reticulum (ER) Stress Inducers.

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Cl--ion transporters (2a-2h) were synthesized based on the binding motifs of prodigiosin. Transporter 2e clearly displays Cl--ion transportation activity across both model and live cell membranes. Furthermore, 2e can disrupt… Click to show full abstract

Cl--ion transporters (2a-2h) were synthesized based on the binding motifs of prodigiosin. Transporter 2e clearly displays Cl--ion transportation activity across both model and live cell membranes. Furthermore, 2e can disrupt Ca2+ homeostasis and increase the intracellular concentration of Ca2+ in the DLD-1 cell. This disruption can lead to Caspase-dependent apoptosis supported by CHOP expression (a marker of ER stress) and the appearance of the cleaved forms of Caspase 3 and PARP.

Keywords: transporters endoplasmic; synthetic anion; endoplasmic reticulum; reticulum stress; stress; anion transporters

Journal Title: Organic letters
Year Published: 2019

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