Synthetic anion transporters as endoplasmic reticulum (ER) stress inducers

AS Aslam, A Fuwad, H Ryu, B Selvaraj, JW Song… - Organic …, 2019 - ACS Publications
AS Aslam, A Fuwad, H Ryu, B Selvaraj, JW Song, DW Kim, SM Kim, JW Lee, TJ Jeon
Organic letters, 2019ACS Publications
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.
Cl-ion transporters (2a2h) 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.
ACS Publications
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