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PERK inhibitors

PERK inhibitors are compounds designed to target and inhibit the protein kinase RNA-like endoplasmic reticulum kinase (PERK). PERK is a key regulator of the unfolded protein response (UPR) pathway, which is activated in response to endoplasmic reticulum (ER) stress caused by protein misfolding or accumulation. During ER stress, PERK phosphorylates the eukaryotic initiation factor 2 alpha (eIF2α), leading to attenuation of protein synthesis and reducing the load of unfolded proteins in the ER. This adaptive response helps restore ER homeostasis and promote cell survival under stress conditions. However, persistent activation of PERK and the UPR pathway can contribute to chronic inflammation, cell death, and promote tumor growth in cancer cells. By inhibiting PERK, PERK inhibitors aim to block this pathway, potentially sensitizing cancer cells to apoptosis and reducing tumor growth.
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