YM155 (YM-155, Sepantronium Bromide)是一种新型的小分子survivin抑制剂(生存素抑制剂、存活素抑制剂),IC50为0.54 nM,通过抑制survivin基因启动子转录从而抑制survivin表达,而不会显著抑制SV40启动子活性。YM155具有抗肿瘤活性,通过激活DNA损伤通路,诱导DNA损伤,从而有效杀死急性淋巴细胞白血病细胞,另外,在多种肿瘤细胞体内外研究中,YM155表现出诱导细胞凋亡,抑制肿瘤生长的作用。
参考文献
[1] Nakahara, T., et al. YM155, a Novel Small-Molecule Survivin Suppressant, Induces Regression of Established Human Hormone-Refractory Prostate Tumor Xenografts. Cancer Res 67: 8014-8021(2007).
[2] Nakahara, T., et al. Broad spectrum and potent antitumor activities of YM155, a novel small-molecule survivin suppressant, in a wide variety of human cancer cell lines and xenograft models. Cancer Sci. 102(3): 614–621(2011).
[3] Iwasa, T., et al. Radiosensitizing Effect of YM155, a Novel Small-Molecule Survivin Suppressant, in Non-Small Cell Lung Cancer Cell Lines. Clin Cancer Res. 14:6496-6504 (2008).
[4] Bill H Chang, et al. YM155 potently kills acute lymphoblastic leukemia cells through activation of the DNA damage pathway. Journal of Hematology & Oncology 8:39 (2015).
[5] Yan-Fang Tao, et al. Survivin selective inhibitor YM155 induce apoptosis in SK-NEP-1 Wilms tumor cells. BMC Cancer 12:619 (2012)
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