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- W2910810461 abstract "Bone metastasis is a major cause of prostate cancer (PCa) mortality. Although docetaxel chemotherapy initially extends patients’ survival, in most cases PCa becomes chemoresistant and eventually progresses without a cure. In this study, we developed a novel small-molecule compound BKM1972, which exhibited potent in vitro cytotoxicity in PCa and other cancer cells regardless of their differences in chemo-responsiveness. Mechanistic studies demonstrated that BKM1972 effectively inhibited the expression of anti-apoptotic protein survivin and membrane-bound efflux pump ATP binding cassette B 1 (ABCB1, p-glycoprotein), presumably via signal transducer and activator of transcription 3 (Stat3). BKM1972 was well tolerated in mice and as a monotherapy, significantly inhibited the intraosseous growth of chemosensitive and chemoresistant PCa cells. These results indicate that BKM1972 is a promising small-molecule lead to treat PCa bone metastasis and overcome docetaxel resistance." @default.
- W2910810461 created "2019-01-25" @default.
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- W2910810461 date "2019-04-01" @default.
- W2910810461 modified "2023-10-18" @default.
- W2910810461 title "Small molecule BKM1972 inhibits human prostate cancer growth and overcomes docetaxel resistance in intraosseous models" @default.
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- W2910810461 doi "https://doi.org/10.1016/j.canlet.2019.01.010" @default.
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