| Autor: |
Kai-long Jiang, Chang-mei Liu, Li-tong Nie, Hai-ni Jiang, Lei Xu, Kun-zhi Zhang, Li-xia Fan, An-hui Gao, Lu-ling Lin, Xiang-yu Wang, Ming-jia Tan, Qi-qing Zhang, Yu-bo Zhou, Jia Li |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
Acta pharmacologica Sinica. 44(1) |
| ISSN: |
1745-7254 |
| Popis: |
Inositol-requiring enzyme 1α (IRE1α) is the most conserved endoplasmic reticulum (ER) stress sensor with two catalytic domains, kinase and RNase, in its cytosolic portion. IRE1α inhibitors have been used to improve existing clinical treatments against various cancers. In this study we identified toxoflavin (TXF) as a new-type potent small molecule IRE1α inhibitor. We used luciferase reporter systems to screen compounds that inhibited the IRE1α-XBP1s signaling pathway. As a result, TXF was found to be the most potent IRE1α RNase inhibitor with an IC |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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