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发明公开
CN108785310A 凡德他尼在制备靶向EphB4的抗肿瘤药物中的应用 无效 - 驳回

凡德他尼在制备靶向EphB4的抗肿瘤药物中的应用
摘要：
本发明公开了凡德他尼(dasatinib)在制备靶向EphB4的抗肿瘤药物中的应用，属于医药技术领域。本发明通过实验验证凡德他尼的上述应用，分子对接法、SPR法和MST实验结果表明凡德他尼能够与EphB4相互作用。EphB4激酶实验显示，凡德他尼可明显抑制EphB4激酶活性。显著抑制白血病细胞K562，JLTRG，H9的增殖。同时，凡德他尼显著抑制EphB4下游的信号分子p‑PI3K p85/p55、PI3K p85表达，下调MEK和ERK的磷酸化水平。因此，本发明的实验结果充分支持凡德他尼在抗白血病药物和靶向EphB4的肿瘤药物中的应用。
摘要（英）：

The invention discloses an application of Vandetanib to preparation of a targeted EphB4 anti-tumor drug, and belongs to the technical field of medicines. Experiments verify the application of the Vandetanib, and a molecular docking method, an SPR (surface plasmon resonance) method and MST (modulated scatterer technique) experiment results indicate that the Vandetanib can interact with EphB4. EphB4kinase experiments display that the Vandetanib can obviously inhibit EphB4 kinase activity. Proliferation of leukemic cells K562, JLTRG and H9 is remarkably inhibited. Besides, the Vandetanib remarkably inhibits expression of signal molecules p-PI3K p85/p55 and PI3K p85 at the downstream of the EphB4, and the phosphorylation level of MEK (methyl ethyl ketone) and ERK (extracellular signal-regulated kinase) is reduced. Therefore, the experiment results sufficiently support the application of the Vandetanib to an anti-leukemia drug and the targeted EphB4 anti-tumor drug.

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