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YM155对透明细胞肾细胞癌的作用不依赖于生存素表达水平。

Action of YM155 on clear cell renal cell carcinoma does not depend on survivin expression levels.

作者信息

Sim Mei Yi, Huynh Hung, Go Mei Lin, Yuen John Shyi Peng

机构信息

Department of Urology, Singapore General Hospital, Republic of Singapore.

Laboratory of Molecular Endocrinology, Division of Molecular and Cellular Research, National Cancer Centre, Republic of Singapore.

出版信息

PLoS One. 2017 Jun 5;12(6):e0178168. doi: 10.1371/journal.pone.0178168. eCollection 2017.

Abstract

The dioxonapthoimidazolium YM155 is a survivin suppressant which has been investigated as an anticancer agent in clinical trials. Here, we investigated its growth inhibitory properties on a panel of immortalized and patient derived renal cell carcinoma (RCC) cell lines which were either deficient in the tumour suppressor von Hippel-Lindau (VHL) protein or possessed a functional copy. Neither the VHL status nor the survivin expression levels of these cell lines influenced their susceptibility to growth inhibition by YM155. Of the various RCC lines, the papillary subtype was more resistant to YM155, suggesting that the therapeutic efficacy of YM155 may be restricted to clear cell subtypes. YM155 was equally potent in cells (RCC786.0) in which survivin expression had been stably silenced or overexpressed, implicating a limited reliance on survivin in the mode of action of YM155. A follow-up in-vitro high throughput RNA microarray identified possible targets of YM155 apart from survivin. Selected genes (ID1, FOXO1, CYLD) that were differentially expressed in YM155-sensitive RCC cells and relevant to RCC pathology were validated with real-time PCR and western immunoblotting analyses. Thus, there is corroboratory evidence that the growth inhibitory activity of YM155 in RCC cell lines is not exclusively mediated by its suppression of survivin. In view of the growing importance of combination therapy in oncology, we showed that a combination of YM155 and sorafenib at ½ x IC50 concentrations was synergistic on RCC786.0 cells. However, when tested intraperitoneally on a murine xenograft model derived from a nephrectomised patient with clear cell RCC, a combination of suboptimal doses of both drugs failed to arrest tumour progression. The absence of synergy in vivo highlighted the need to further optimize the dosing schedules of YM155 and sorafenib, as well as their routes of administration. It also implied that the expression of other oncogenic proteins which YM155 may target is either low or absent in this clear cell RCC.

摘要

二氧萘并咪唑啉盐YM155是一种survivin抑制剂,已作为抗癌药物进行临床试验研究。在此,我们研究了它对一组永生化和患者来源的肾细胞癌(RCC)细胞系的生长抑制特性,这些细胞系要么缺乏肿瘤抑制因子希佩尔-林道(VHL)蛋白,要么拥有功能性拷贝。这些细胞系的VHL状态和survivin表达水平均不影响它们对YM155生长抑制的敏感性。在各种RCC细胞系中,乳头状亚型对YM155更具抗性,这表明YM155的治疗效果可能仅限于透明细胞亚型。YM155在survivin表达稳定沉默或过表达的细胞(RCC786.0)中同样有效,这表明YM155的作用模式对survivin的依赖性有限。后续的体外高通量RNA微阵列分析确定了除survivin之外YM155可能的靶点。通过实时PCR和western免疫印迹分析验证了在YM155敏感的RCC细胞中差异表达且与RCC病理相关的选定基因(ID1、FOXO1、CYLD)。因此,有确凿证据表明YM155在RCC细胞系中的生长抑制活性并非仅由其对survivin的抑制介导。鉴于联合治疗在肿瘤学中的重要性日益增加,我们表明YM155和索拉非尼在½ x IC50浓度下联合对RCC786.0细胞具有协同作用。然而,当在源自一名肾切除的透明细胞RCC患者的小鼠异种移植模型上进行腹腔内测试时,两种药物的次优剂量联合未能阻止肿瘤进展。体内缺乏协同作用突出了进一步优化YM155和索拉非尼给药方案及其给药途径的必要性。这也意味着在这种透明细胞RCC中,YM155可能靶向的其他致癌蛋白的表达要么很低,要么不存在。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4e9/5459331/bc76ad98baa7/pone.0178168.g001.jpg

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