Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation
書誌事項
- 公開日
- 2015-10
- 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
-
- 10.1016/j.bmc.2015.08.042
- 公開者
- Elsevier BV
この論文をさがす
説明
Protein phosphatase magnesium-dependent 1δ (PPM1D, Wip1) is a p53 inducible serine/threonine phosphatase. PPM1D is a promising target protein in cancer therapy since overexpression, missense mutations, truncating mutations, and gene amplification of PPM1D are reported in many tumors, including breast cancer and neuroblastoma. Herein, we report that a specific inhibitor, SL-176 that can be readily synthesized in 10 steps, significantly inhibits proliferation of a breast cancer cell line overexpressing PPM1D and induces G2/M arrest and apoptosis. SL-176 decreases PPM1D enzyme activity potently and specifically in vitro. These results demonstrate that SL-176 could be a useful lead compound in the development of effective anti-cancer agents.
収録刊行物
-
- Bioorganic & Medicinal Chemistry
-
Bioorganic & Medicinal Chemistry 23 (19), 6246-6249, 2015-10
Elsevier BV
