Department of Urology, The Second Affiliated Hospital of Soochow University, Suzhou, Jiangsu 215004, P.R. China.
Department of Urology, The Affiliated Suzhou Hospital of Nanjing Medical University, Suzhou Municipal Hospital, Suzhou, Jiangsu 215008, P.R. China.
Oncol Rep. 2021 Mar;45(3):963-974. doi: 10.3892/or.2021.7925. Epub 2021 Jan 5.
The human testicular nuclear receptor 4 (TR4) is a critical regulatory gene for the progression of prostate cancer (PCa). Although it has been revealed that TR4 causes chemoresistance in PCa via the activation of octamer‑binding transcription factor 4 (OCT4), the detailed mechanism remains unexplored. In the present study, it was revealed that inhibition of TR4 by shRNA in PCa enhanced the sensitivity to docetaxel in vitro and in vivo. TR4 induced the downregulation of miR‑145 by directly binding it to the promoter of miR‑145, which was confirmed by chromatin immunoprecipitation analysis and luciferase assay. The overexpression of miR‑145 suppressed both the chemoresistance and the expression of OCT4 mRNA and protein. Additionally, the TR4 shRNA mediated re‑sensitization to docetaxel, along with the downregulated expression of OCT4, were reversed by the concurrent inhibition of miR‑145. The luciferase assay revealed that the activity of the wild‑type OCT4 3' untranslated region reporter was suppressed. This suppression diminished when the miR‑145 response element mutated. These findings suggest an undescribed regulatory pathway in PCa, by which TR4 directly suppressed the expression of miR‑145, thereby inhibiting its direct target OCT4, leading to the promotion of chemoresistance in PCa.
人类睾丸核受体 4(TR4)是前列腺癌(PCa)进展的关键调节基因。虽然已经揭示 TR4 通过激活八聚体结合转录因子 4(OCT4)导致 PCa 的化学抗性,但详细的机制仍未被探索。在本研究中,通过 shRNA 抑制 PCa 中的 TR4 增强了体外和体内对多西他赛的敏感性。TR4 通过直接结合 miR-145 的启动子,诱导 miR-145 的下调,染色质免疫沉淀分析和荧光素酶测定证实了这一点。miR-145 的过表达抑制了化学抗性和 OCT4 mRNA 和蛋白的表达。此外,TR4 shRNA 介导的对多西他赛的重新敏感性,以及 OCT4 的下调表达,可被同时抑制 miR-145 逆转。荧光素酶测定显示野生型 OCT4 3'非翻译区报告基因的活性受到抑制。当 miR-145 反应元件发生突变时,这种抑制作用减弱。这些发现提示了 PCa 中一种未描述的调节途径,其中 TR4 直接抑制 miR-145 的表达,从而抑制其直接靶标 OCT4,导致 PCa 中化学抗性的增强。