A small molecule inhibitor of p53-inducible protein phosphatase PPM1D
書誌事項
- 公開日
- 2012-01
- 資源種別
- journal article
- 権利情報
-
- https://www.elsevier.com/tdm/userlicense/1.0/
- https://www.elsevier.com/legal/tdmrep-license
- DOI
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- 10.1016/j.bmcl.2011.10.084
- 公開者
- Elsevier BV
この論文をさがす
説明
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.
収録刊行物
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- Bioorganic & Medicinal Chemistry Letters
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Bioorganic & Medicinal Chemistry Letters 22 (1), 729-732, 2012-01
Elsevier BV
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キーワード
- Indoles
- Time Factors
- Proto-Oncogene Proteins pp60(c-src)
- Antineoplastic Agents
- Apoptosis
- Cell Cycle Proteins
- Ataxia Telangiectasia Mutated Proteins
- Protein Serine-Threonine Kinases
- Inhibitory Concentration 50
- Cell Line, Tumor
- Neoplasms
- Phosphoprotein Phosphatases
- Humans
- Phosphorylation
- Cell Proliferation
- Dose-Response Relationship, Drug
- Tumor Suppressor Proteins
- Phenanthrenes
- Phosphoric Monoester Hydrolases
- DNA-Binding Proteins
- Protein Phosphatase 2C
- Models, Chemical
- Tumor Suppressor Protein p53
詳細情報 詳細情報について
-
- CRID
- 1360002215833699456
-
- ISSN
- 0960894X
-
- PubMed
- 22115592
-
- 資料種別
- journal article
-
- データソース種別
-
- Crossref
- KAKEN
- OpenAIRE
