Synthetic Anion Transporters as Endoplasmic Reticulum (ER) Stress Inducers

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 th...

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Bibliographic Details
Published in:Organic letters 2019-10, Vol.21 (19), p.7828-7832
Main Authors: Aslam, Adil S, Fuwad, Ahmed, Ryu, Hyunil, Selvaraj, Baskar, Song, Jae-Won, Kim, Dae Won, Kim, Sun Min, Lee, Jae Wook, Jeon, Tae-Joon, Cho, Dong-Gyu
Format: Article
Language:English
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Summary: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.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.9b02823