期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 1, 页码 729-732出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.10.084
关键词
Inhibitor; Phosphatase; Dephosphorylation; Apoptosis; Anti-tumor agent
资金
- JSPS [21310133, 17750148, 20770095, 22 . 1998]
- MEXT [12213105, 13214079]
- Grants-in-Aid for Scientific Research [20770095, 21106010, 10J01998, 21310133, 12213105, 23651210, 22710206, 13214079, 17750148] Funding Source: KAKEN
PPM1D is a p53-inducible Ser/Thr protein phosphatase. PPM1D gene amplification and overexpression have been reported in a variety of human tumors, including breast cancer and neuroblastoma. Because the phosphatase activity of PPM1D is essential for its oncogenic role, PPM1D inhibitors should be viable anti-cancer agents. In our current study, we showed that SPI-001 was a potent and specific PPM1D inhibitor. SPI-001 inhibited PPM1D phosphatase activity in PPM1D-overexpressing human breast cancer cells and increased phosphorylation of p53. Furthermore, SPI-001 suppressed cell proliferation by inducing apoptosis. Our present study suggested that SPI-001 was a potential lead compound in developing anti-cancer drugs. (C) 2011 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据