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YM155 enhances docetaxel efficacy in ovarian cancer.YM155增强多西他赛对卵巢癌的疗效。
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2
Generation of reactive oxygen species is the primary mode of action and cause of survivin suppression by sepantronium bromide (YM155).活性氧的产生是溴化司帕沙星（YM155）抑制生存素的主要作用方式和原因。
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Adaptation to chronic exposure to sepantronium bromide (YM155), a prototypical survivin suppressant is due to persistent DNA damage-response in breast cancer cells.对慢性暴露于溴化司帕托onium（YM155）（一种典型的survivin抑制剂）的适应是由于乳腺癌细胞中持续的DNA损伤反应。
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The survivin suppressant YM155 reverses doxorubicin resistance in osteosarcoma.生存素抑制剂YM155可逆转骨肉瘤对多柔比星的耐药性。
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YM155 sensitizes HeLa cells to TRAIL-mediated apoptosis via cFLIP and survivin downregulation.YM155通过下调cFLIP和survivin使HeLa细胞对TRAIL介导的凋亡敏感。
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Surviving Inhibition Induces Cell Cycle Arrest and Disrupts Multipotency in Haemangioma Stem Cells.抗血管生成治疗诱导血管瘤干细胞周期阻滞和多能性丧失
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Survivin Interference and SurVaxM as an Adjunct Therapy for Glioblastoma Multiforme.生存素干扰与SurVaxM作为多形性胶质母细胞瘤的辅助治疗方法
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Hsa_circ_0006404 and hsa_circ_0000735 Regulated Ovarian Cancer Response to Docetaxel Treatment via Regulating p-GP Expression.Hsa_circ_0006404 和 hsa_circ_0000735 通过调节 p-GP 表达调控卵巢癌细胞对多西他赛治疗的反应。
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Emerging Effects of Sepantronium Bromide (YM155) on MOLT-4 Cell Line Apoptosis Induction and Expression of Critical Genes Involved in Apoptotic Pathways.溴化塞帕替尼（YM155）对MOLT-4细胞系凋亡诱导及凋亡途径相关关键基因表达的新作用
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本文引用的文献

1
Volasertib suppresses the growth of human hepatocellular carcinoma and .沃拉塞替布抑制人肝癌细胞的生长并且……（原文此处不完整）
Am J Cancer Res. 2016 Nov 1;6(11):2476-2488. eCollection 2016.
2
Effects of YM155 on survivin levels and viability in neuroblastoma cells with acquired drug resistance.YM155对获得性耐药神经母细胞瘤细胞中生存素水平及活力的影响。
Cell Death Dis. 2016 Oct 13;7(10):e2410. doi: 10.1038/cddis.2016.257.
3
Targeting ABCB1-mediated tumor multidrug resistance by CRISPR/Cas9-based genome editing.通过基于CRISPR/Cas9的基因组编辑靶向ABCB1介导的肿瘤多药耐药性。
Am J Transl Res. 2016 Sep 15;8(9):3986-3994. eCollection 2016.
4
Wallichinine reverses ABCB1-mediated cancer multidrug resistance.瓦立千里光宁碱可逆转ABCB1介导的癌症多药耐药性。
Am J Transl Res. 2016 Jul 15;8(7):2969-80. eCollection 2016.
5
Volasertib suppresses tumor growth and potentiates the activity of cisplatin in cervical cancer.沃拉替尼抑制宫颈癌的肿瘤生长并增强顺铂的活性。
Am J Cancer Res. 2015 Nov 15;5(12):3548-59. eCollection 2015.
6
Sequential combination therapy of ovarian cancer with cisplatin and γ-secretase inhibitor MK-0752.顺铂联合γ-分泌酶抑制剂 MK-0752 治疗卵巢癌。
Gynecol Oncol. 2016 Mar;140(3):537-44. doi: 10.1016/j.ygyno.2015.12.011. Epub 2015 Dec 15.
7
Synergistic anticancer effects of triptolide and celastrol, two main compounds from thunder god vine.雷公藤两种主要化合物雷公藤内酯醇和雷公藤红素的协同抗癌作用
Oncotarget. 2015 Oct 20;6(32):32790-804. doi: 10.18632/oncotarget.5411.
8
Breast cancer cells respond differently to docetaxel depending on their phenotype and on survivin upregulation.乳腺癌细胞对多西他赛的反应因其表型和生存素上调情况而异。
Tumour Biol. 2016 Feb;37(2):2603-11. doi: 10.1007/s13277-015-4075-x. Epub 2015 Sep 21.
9
Phase II, multicenter, open-label, randomized study of YM155 plus docetaxel as first-line treatment in patients with HER2-negative metastatic breast cancer.YM155联合多西他赛作为HER2阴性转移性乳腺癌患者一线治疗的多中心、开放标签、随机II期研究。
Breast Cancer Res Treat. 2015 Jan;149(1):171-9. doi: 10.1007/s10549-014-3238-6. Epub 2014 Dec 30.
10
A phase 2, multicenter, open-label study of sepantronium bromide (YM155) plus docetaxel in patients with stage III (unresectable) or stage IV melanoma.一项关于溴化塞潘托铵（YM155）联合多西他赛用于III期（不可切除）或IV期黑色素瘤患者的2期、多中心、开放标签研究。
Cancer Med. 2015 May;4(5):643-50. doi: 10.1002/cam4.363. Epub 2014 Dec 23.

YM155增强多西他赛对卵巢癌的疗效。

YM155 enhances docetaxel efficacy in ovarian cancer.

作者信息

Hou Li-Jiao, Huang Xiao-Xiu, Xu Li-Na, Zhang Yan-Yan, Zhao Na, Ou Rong-Ying, Li Wen-Feng, Zhang Wen-Ji, Jiang Qi-Wei, Yang Yang, Wei Meng-Ning, Huang Jia-Rong, Wang Kun, Yuan Meng-Ling, Xing Zi-Hao, Shi Zhi, Yan Xiao-Jian

机构信息

Department of Gynecology, The First Affiliated Hospital of Wenzhou Medical UniversityWenzhou 325000, Zhejiang, China.

Department of Chemoradiotherapy, The First Affiliated Hospital of Wenzhou Medical UniversityWenzhou 325000, Zhejiang, China.

出版信息

Am J Transl Res. 2018 Mar 15;10(3):696-708. eCollection 2018.

PMID:29636860
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5883111/
Abstract

YM155 (Sepantronium bromide) is a potent small molecule inhibitor of survivin by suppression of survivin expression and shows the promising anticancer activity in many types of cancers. Docetaxel (Taxotere) is a member of the taxane drugs used in the treatment of a number of cancers in clinic. Despite the therapeutic efficacy of docetaxel is encouraging, the emergent resistance is an urgent issue. In this study, we investigate the effect of YM155 on docetaxel efficacy in ovarian cancer cells. Our data showed that YM155 actively induced cell growth inhibition, cell cycle arrest and apoptosis with downregualtion of survivin in ovarian cancer cells. Moreover, YM155 increased the intracellular ROS levels, and pretreatment with either NAC or GSH partially reversed the YM155-induced ROS accumulation and apoptosis only in the parental A2780 cells, but not in the resistant A2780/Taxol cells. Furthermore, YM155 enhanced docetaxel efficacy to inhibit the growth and induce apoptosis in ovarian cancer cells. Take together, our results suggested that combination of YM155 and docetaxel may be a feasible strategy for the treatment of ovarian cancer.

摘要

YM155（溴化司帕沙星）是一种通过抑制生存素表达而发挥作用的强效小分子生存素抑制剂，在多种癌症中显示出有前景的抗癌活性。多西他赛（泰索帝）是临床上用于治疗多种癌症的紫杉烷类药物成员之一。尽管多西他赛的治疗效果令人鼓舞，但出现的耐药性是一个紧迫问题。在本研究中，我们探究了YM155对卵巢癌细胞中多西他赛疗效的影响。我们的数据表明，YM155能在卵巢癌细胞中通过下调生存素，积极诱导细胞生长抑制、细胞周期阻滞和凋亡。此外，YM155增加细胞内活性氧水平，用NAC或GSH预处理仅在亲代A2780细胞中部分逆转了YM155诱导的活性氧积累和凋亡，而在耐药的A2780/紫杉醇细胞中则没有。此外，YM155增强了多西他赛抑制卵巢癌细胞生长和诱导凋亡的疗效。综上所述，我们的结果表明，YM155与多西他赛联合使用可能是治疗卵巢癌的一种可行策略。