Synthetic Anion Transporters as Endoplasmic Reticulum (ER) Stress Inducers

Org Lett. 2019 Oct 4;21(19):7828-7832. doi: 10.1021/acs.orglett.9b02823. Epub 2019 Sep 3.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calcium / analysis
  • Calcium / metabolism
  • Cell Line, Tumor
  • Cell Membrane / drug effects
  • Endoplasmic Reticulum / drug effects
  • Endoplasmic Reticulum / metabolism
  • Endoplasmic Reticulum Stress / drug effects
  • Humans
  • Molecular Structure
  • Organic Anion Transporters / chemical synthesis
  • Organic Anion Transporters / chemistry
  • Organic Anion Transporters / pharmacology*
  • Prodigiosin / chemical synthesis
  • Prodigiosin / chemistry
  • Prodigiosin / pharmacology*

Substances

  • Organic Anion Transporters
  • Prodigiosin
  • Calcium