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• W4294716489 abstract "Prostate cancer (CaP) is one of the most frequent malignancies amongst men. Enzalutamide is the second-generation potent androgen receptor (AR) antagonist used against metastatic and non-metastatic CaP. Unfortunately, the development of chemoresistance in cancer cells reduces the effectiveness of Enzalutamide. Lupeol is a pentacyclic triterpene found in different fruits, vegetables, and medicinal plants and possesses anti-inflammatory and anti-cancer properties. Here, we report in silico and in vitro studies of Lupeol and Enzalutamide against the β-CATENIN, c-FLIPL, and c-MYC, which play a significant role in chemoresistance. We observed that Lupeol significantly inhibits the cell growth of chemoresistant Du145 cells and cancer stem cells (CSCs) either alone or in combination with Enzalutamide. Lupeol and Enzalutamide were also found to dock with β-CATENIN, c-FLIPL, and c-MYC. The following MD simulation data showed both compounds exerting structural changes in these proteins. Finally, they significantly inhibit the transcriptional activity of all these genes, as observed by luciferase assay. Thus, we infer that Lupeol chemosensitizes the CaP cells for Enzalutamide-resistant CaP cells." @default.
• W4294716489 created "2022-09-06" @default.
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• W4294716489 date "2022-09-04" @default.
• W4294716489 modified "2023-10-10" @default.
• W4294716489 title "Role of lupeol in chemosensitizing therapy-resistant prostate cancer cells by targeting MYC, β-catenin and c-FLIP: in silico and in vitro studies" @default.
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• W4294716489 doi "https://doi.org/10.1007/s40203-022-00131-3" @default.
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