已显示eIF4E / eIF4G相互作用抑制剂4EGI-1可通过FLIP | S / L |的下调和DR5的诱导来扩增TRAIL(肿瘤坏死因子相关的凋亡诱导配体)诱导的凋亡。该化合物的这些特征似乎与其抑制帽依赖性蛋白质翻译的能力无关,后者是由于通过与eIF4E结合而破坏eIF4E / eIF4G缔合而引起的。已经表明,尽管4EGI-1从eIF4E置换出eIF4G,但其却同时增强了体内和体外的4E-BP缔合。4E-BPs调节了eIF4E / eIF4G复合体,该复合体在翻译起始水平上对基因表达的调控中起着核 eIF4E/eIF4G Interaction Inhibitor, 4EGI-1, has been shown to amplify TRAIL (tumor necrosis factor-related apoptosis-inducing ligand)-induced apoptosis via down-regulation of FLIP|S/L|and induction of DR5. These characteristics of the compound seem to be independent of it′s ability to inhibit cap-dependent protein translation which is caused by disruption of the eIF4E/eIF4G association through binding to eIF4E. It has been shown that while 4EGI-1 displaces eIF4G from eIF4E, it consequentially enhances 4E-BP association both|in vivo|and|in vitro|. 4E-BPs regulated the eIF4E/eIF4G complex which has a central role in the regulation of gene expression at the level of translation initiation.
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eIF4E/eIF4G Interaction Inhibitor, 4EGI-1
CAS number:315706-13-9 molecular formula:C18H12Cl2N4O4S
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| Chinese alias | eIF4E/eIF4G 相互作用抑制剂,4EGI-1 | ||
| English alias | - | ||
| CAS number | 315706-13-9 | molecular formula | C18H12Cl2N4O4S |
| molecular weight | 451.28 g/mol | Exact mass | 10mM in DMSO |
| PSA | 149.000 Ų | logp | 6.100 |
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