Phosphorylation of eukaryotic initiation factor-2α (eIF2α) in …
2020年6月8日 · An inhibitor of HIV-1 protease modulates constitutive eIF2alpha dephosphorylation to trigger a specific integrated stress response. Proc. Natl Acad. Sci. USA 113 , E117–E126 (2016).
The small molecule ISRIB reverses the effects of eIF2α …
Although there are inhibitors of specific eIF2α kinases (PERK and PKR inhibitors), ISRIB is the only molecule that can block signaling downstream of all eIF2α kinases by making cells resistant to eIF2α phosphorylation.
Inhibition of EIF2α Dephosphorylation Decreases Cell Viability and ...
2023年11月9日 · Inhibition of EIF2α dephosphorylation decreases HNSCC cell viability and clonogenic survival and impairs the G 1 /S transition. Salubrinal also decreases the viability of PD3DS and acts synergistically with cisplatin, 5-fluorouracil, bleomycin, …
A selective inhibitor of eIF2alpha dephosphorylation protects cells ...
2005年2月11日 · In a screen for small molecules that protect cells from endoplasmic reticulum (ER) stress, we identified salubrinal, a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit alpha (eIF2alpha).
Increased levels of eIF2A inhibit translation by sequestering 40S ...
2023年10月10日 · To decipher which step of translation is being inhibited by eIF2A, we used sucrose gradient ultracentrifugation along with various translation inhibitors to capture and measure the levels of translation complexes at different stages on nLuc reporter mRNA.
A Selective Inhibitor of eIF2α Dephosphorylation Protects
2005年2月11日 · These results suggest that selective chemical inhibitors of eIF2α dephosphorylation may be useful in diseases involving ER stress or viral infection. More broadly, salubrinal demonstrates the feasibility of selective pharmacological targeting of cellular dephosphorylation events.
Inhibition of the integrated stress response by viral proteins …
2020年7月20日 · We now describe two viral proteins—one from a coronavirus and the other from a picornavirus—that have independently acquired the ability to counteract the ISR at its very core by acting as a...
Blocking UV-Induced eIF2α Phosphorylation with Small Molecule ...
We describe herein the identification of three small-molecule inhibitors of the eIF2α kinase GCN2 that inhibit eIF2α phosphorylation in vitro and in vivo. SP600125 was originally identified from a screen for Jun N-terminal kinase inhibitor and found to target proteins of that family .
Inhibition of eIF2α dephosphorylation enhances TRAIL-induced
2014年2月13日 · Here, we investigate the effects of inhibition of eukaryotic initiation factor 2 subunit α (eIF2 α) dephosphorylation on TRAIL-induced apoptosis in hepatoma cells.
New activators of eIF2α Kinase Heme-Regulated Inhibitor (HRI) …
2020年2月1日 · Heme-regulated inhibitor (HRI), a eukaryotic translation initiation factor 2 alpha (eIF2α) kinase, is critically important for coupling protein synthesis to heme availability in reticulocytes and adaptation to various environmental stressors in all cells.