Development of radiation-sensitizing anti-cancer agents using G2 checkpoint aberogator

本研究旨在探讨G2检查点抑制剂对实体肿瘤的辐射增敏作用，发现一种既能提高肿瘤放疗疗效又能减少肿瘤放疗不良反应的新型抗癌药物。我们研究了各种G2检查点抑制剂对食管癌TE5细胞株x射线照射诱导G2阻滞和抗增殖作用的影响。细胞周期分析和台盼蓝排除实验表明，UCN-01分别消除了G2阻滞和增强了生长抑制。此外，Western blotting结果显示UCN-01降低x射线照射激活的Chk1激酶蛋白水平。

The present study aims at examing the radiation-sensitizing effect of G2 checkpoint abrogators against solid cancers and discovering the new anti-cancer agent which brings both benefits, enhancing the therapeutic efficacy and decreasing adverse effects of cancer radiotherapy. We examined the effects of various G2 checkpoint abrogators on G2 arrest induction and antiproliferative effect by X-ray irradiation against esophageal cancer cell line, TE5. Cell cycle analysis and trypan blue exclusion assay showed that UCN-01 abrogated G2 arrest and potentiated growth inhibition, respectively. Furthermore, Western blotting demonstrated that UCN-01 decreased the protein level of Chk1 kinase activated by X-ray irradiation.