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- W2007183717 abstract "P53 inactivation caused by aberrant expression of its major regulators(e.g, MDM2 and MDMX) contributes to 50% of human cancers. Recent studies have demonstrated that restoration of p53 activity by counteracting p53 repression is a promising anti-cancer strategy. Although agents(e.g., Nutlin-3a) disrupting the MDM2-p53 interaction can inhibit tumor growth, they are less effective in cancer cells with high MDMX expression levels. MDMX binds to p53 and serves as a major p53 antagonist by mainly repressing its transcriptional activity. Here we reported the identification of two samll molecules inhibitory for MDMX expression through high-throughput screening. Treatments of MCF-7 cells with these MDMX inhibitors dramatically increased the stability of p53, leading to elevated expression of proapoptotic genes(e.g., PUMA, Bax, and PIG3). These results argue for a recent notion that MDMX is a major regulator of the p53 stability. While they exerted limited effects on cell cycle progression, this new class of small-molecule p53 activitors induced MCF7 cells to undergo apoptosis. However, the MDMX inhibitors only modestly enhanced p53 activition induced by Nutlin-3a. We conclue that small molecules targeting MDMX expression would be of therapeutic benefits and be useful in dissecting the p53 network through chemical biological approaches. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 101st Annual Meeting of the American Association for Cancer Research; 2010 Apr 17-21; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2010;70(8 Suppl):Abstract nr 4528." @default.
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- W2007183717 date "2010-04-15" @default.
- W2007183717 modified "2023-09-25" @default.
- W2007183717 title "Abstract 4528: Small molecules inhibitory for MDMX expression activate p53 and induce apoptosis" @default.
- W2007183717 doi "https://doi.org/10.1158/1538-7445.am10-4528" @default.
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