(Z)-4EGI-1 是 4EGI-1 的 Z-型异构体，是 eIF4E/eIF4G 相互作用和翻译起始的抑制剂。(Z)-4EGI-1 有效结合 eIF4E ，IC50 为 43.5 μM，Kd 值为 8.74 μM。(Z)-4EGI-1 具有抗癌活性。
(Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity[1][2].
[1]. Khuloud Takrouri, et al. Structure-activity Relationship Study of 4EGI-1, Small Molecule eIF4E/eIF4G Protein-Protein Interaction Inhibitors. Eur J Med Chem. 2014 Apr 22;77:361-77. [2]. Poornachandran Mahalingam, et al. Synthesis of Rigidified eIF4E/eIF4G inhibitor-1 (4EGI-1) Mimetic and Their in Vitro Characterization as Inhibitors of Protein-Protein Interaction. J Med Chem. 2014 Jun 26;57(12):5094-111.
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