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Glycogen synthase kinase 3 (GSK‐3) has been regarded as a potential therapeutic target for multiple human cancers. We previously reported that suppression of GSK‐3 activity with lithium chloride (LiCl) or small chemical inhibitors impaired cellular DNA synthesis and reduced cell proliferation in prostate cancer cells. Therefore, in this study, we extended this in vitro findings to in vivo settings in order to establish a proof of concept that inhibition of GSK‐3 activity is feasible in suppressing tumor growth of prostate cancer in vivo.

In this study, we used three GSK‐3 inhibitors, LiCl, TDZD‐8, and L803‐mts, which are structurally unrelated and non‐ATP competitive. Human prostate cancer cell lines PC‐3 and C4‐2 were used for nude mouse xenograft models. The autochthonous transgenic prostate cancer TRAMP mice were used for testing GSK‐3 inhibitor's effect on tumor development …