Background/aim: To explore the possibility of a selective small-molecule β-catenin inhibitor, CWP232228, as a potential therapeutic drug in the treatment of colorectal cancer (CRC).
Materials And Methods: The effect of CWP2228 on HCT116 cells was analysed in vitro via flow cytometry, western immunoblotting, and luciferase reporter assays. NOD-scid IL2Rgamma mice were employed for an in vivo xenograft study to validate the in vitro studies.
Results: CWP232228 treatment decreased the promoter activity and nuclear expression of β-catenin and induced a significant cytotoxic effect in HCT116 cells. CWP232228 treatment induced apoptosis and cell-cycle arrest in the G phase of the cell cycle. Furthermore, CWP232228 decreased the expression of aurora kinase A, c-Myc, cyclin D1 and microphthalmia-associated transcription factor. Lastly, CWP232228 also inhibited the growth of xenografted colon cancer cells in mice.
Conclusion: Collectively, CWP232228 may be used as a potential therapeutic drug in CRC.
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| http://dx.doi.org/10.21873/anticanres.13514 | DOI Listing |
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