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ID: ALA1938369

Journal: Bioorg Med Chem Lett

Title: A small molecule inhibitor of p53-inducible protein phosphatase PPM1D.

Authors: Yagi H, Chuman Y, Kozakai Y, Imagawa T, Takahashi Y, Yoshimura F, Tanino K, Sakaguchi K.

Abstract: 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.

CiteXplore: 22115592

DOI: 10.1016/j.bmcl.2011.10.084