eif4a 1

Didesmethylrocaglamide, a Rocaglamide derivative, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor that exhibits strong growth-inhibitory effects, with an IC50 of 5 nM. It hinders several growth-promoting signaling pathways and triggers apoptosis in tumor cells, demonstrating antitumor activity[1].

CR-1-31-B, a synthetic rocaglate, acts as a highly potent inhibitor of eIF4A. By disrupting the interaction between eIF4A and RNA, it effectively obstructs the initiation phase of protein synthesis. Specifically, CR-1-31-B interferes with the association between Plasmodium falciparum eIF4A (PfeIF4A) and RNA. Additionally, CR-1-31-B induces apoptosis in neuroblastoma and gallbladder cancer cells [4].

Rocaglamide (Roc-A) 是从米仔兰中分离出来的一种天然产物，具有抗癌特性，可用于咳嗽，受伤，哮喘和炎症性皮肤病。它是一种有效的选择性热休克因子 1 活化抑制剂，IC50约为 50 nM。它是 T 细胞中 NF-κB 活化的有效抑制剂，还抑制翻译起始因子eIF4A 的功能。