Targeting Polo-like Kinase 1 by a Novel Pyrrole-Imidazole Polyamide-Hoechst Conjugate Suppresses Tumor Growth In Vivo.
文献类型：期刊论文
| 作者 | Ding, Zhihao; Liu, Ke; Fang, Lijing; Sun, Haiyan; Pan, Zhengyin; Zhang, Jianchao; Chen, Juntao; Shao, Ximing; Wang, Wei; Tan, Yuanyan |
| 刊名 | MOLECULAR CANCER THERAPEUTICS
 |
| 出版日期 | 2018 |
| 文献子类 | 期刊论文 |
| 英文摘要 | The serine/threonine kinase Polo-like kinase 1 (Plk1) plays a pivotal role in cell proliferation and has been validated as a promising anticancer drug target. However, very limited success has been achieved in clinical applications using existing Plk1 inhibitors, due to lack of sufficient specificity toward Plk1. To develop a novel Plk1 inhibitor with high selectivity and efficacy, we designed and synthesized a pyrrole-imidazole polyamide-Hoechst conjugate, PIP3, targeted to specific DNA sequence in the PLK1 promoter. PIP3 could specifically inhibit the cell cycle-regulated Plk1 expression and consequently retard tumor cell growth. Cancer cells treated with PIP3 exhibited severe mitotic defects and increased apoptosis, whereas normal cells were not affected by PIP3 treatment. Furthermore, subcutaneous injection of PIP3 into mice bearing human cancer xenografts induced significant tumor growth suppression with low host toxicity. Therefore, PIP3 exhibits the potential as an effective agent for targeted cancer therapy |
| URL标识 | 查看原文 |
| 语种 | 英语 |
| 源URL | [http://ir.siat.ac.cn:8080/handle/172644/14593]  |
| 专题 | 深圳先进技术研究院_医药所 |
| 推荐引用方式 GB/T 7714 | Ding, Zhihao,Liu, Ke,Fang, Lijing,et al. Targeting Polo-like Kinase 1 by a Novel Pyrrole-Imidazole Polyamide-Hoechst Conjugate Suppresses Tumor Growth In Vivo.[J]. MOLECULAR CANCER THERAPEUTICS,2018. |
| APA | Ding, Zhihao.,Liu, Ke.,Fang, Lijing.,Sun, Haiyan.,Pan, Zhengyin.,...&Li, Hongchang.(2018).Targeting Polo-like Kinase 1 by a Novel Pyrrole-Imidazole Polyamide-Hoechst Conjugate Suppresses Tumor Growth In Vivo..MOLECULAR CANCER THERAPEUTICS. |
| MLA | Ding, Zhihao,et al."Targeting Polo-like Kinase 1 by a Novel Pyrrole-Imidazole Polyamide-Hoechst Conjugate Suppresses Tumor Growth In Vivo.".MOLECULAR CANCER THERAPEUTICS (2018). |
入库方式： OAI收割
来源：深圳先进技术研究院
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