1.A small molecule UPR modulator for diabetes identified by high throughput screening.
Valeria MARROCCO ; Tuan TRAN ; Siying ZHU ; Seung Hyuk CHOI ; Ana M GAMO ; Sijia LI ; Qiangwei FU ; Marta Diez CUNADO ; Jason ROLAND ; Mitch HULL ; Van NGUYEN-TRAN ; Sean JOSEPH ; Arnab K CHATTERJEE ; Nikki ROGERS ; Matthew S TREMBLAY ; Weijun SHEN
Acta Pharmaceutica Sinica B 2021;11(12):3983-3993
Unfolded protein response (UPR) is a stress response that is specific to the endoplasmic reticulum (ER). UPR is activated upon accumulation of unfolded (or misfolded) proteins in the ER's lumen to restore protein folding capacity by increasing the synthesis of chaperones. In addition, UPR also enhances degradation of unfolded proteins and reduces global protein synthesis to alleviate additional accumulation of unfolded proteins in the ER. Herein, we describe a cell-based ultra-high throughput screening (uHTS) campaign that identifies a small molecule that can modulate UPR and ER stress in cellular and
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