Endocrine Section, Laboratory of Clinical Investigation, National Center for Complementary and Alternative Medicine, National Institutes of Health, Bethesda, Maryland 20892, USA.
Endocrinology. 2010 Apr;151(4):1428-40. doi: 10.1210/en.2009-0885. Epub 2010 Feb 22.
beta-Catenin/T-cell factor signaling (beta-CTS) plays multiple critical roles in carcinogenesis and is blocked by androgens in androgen receptor (AR)-responsive prostate cancer (PrCa) cells, primarily via AR sequestration of beta-catenin from T-cell factor. Dehydroepiandrosterone (DHEA), often used as an over-the-counter nutritional supplement, is metabolized to androgens and estrogens in humans. The efficacy and safety of unregulated use of DHEA are unclear. We now report that DHEA induces beta-CTS via increasing association of estrogen receptor (ER)-beta with Dishevelled2 (Dvl2) in AR nonresponsive human PrCa DU145 cells, a line of androgen-independent PrCa (AiPC) cells. The induction is temporal, as assessed by measuring kinetics of the association of ERbeta/Dvl2, protein expression of the beta-CTS targeted genes, c-Myc and cyclin D1, and cell growth. However, in PC-3 cells, another human AiPC cell line, DHEA exerts no detectible effects, partly due to their lower expression of Galpha-subunits and DHEA down-regulation of ERbeta/Dvl2 association. When Galphaq is overexpressed in PC-3 cells, beta-CTS is constitutively induced, including increasing c-Myc and cyclin D1 protein expression. This effect involved increasing associations of Galphaq/Dvl2 and ERbeta/Dvl2 and promoted cell growth. These activities require ERbeta in DU-145 and PC-3 cells because they are blocked by ICI 182-780 treatment inactivating ERbeta, small interfering RNA administration depleting ERbeta, or AR overexpression arresting ERbeta. These data suggest that novel pathways activating beta-CTS play roles in the progression of AiPC. Although DHEA may enhance PrCa cell growth via androgenic or estrogenic pathways, the effects of DHEA administration on clinical prostate function remain to be determined.
β-连环蛋白/T 细胞因子信号转导 (β-CTS) 在致癌作用中发挥多种关键作用,雄激素受体 (AR) 反应性前列腺癌 (PrCa) 细胞中的雄激素可阻断该信号转导,主要通过 AR 将β-连环蛋白从 T 细胞因子上隔离。脱氢表雄酮 (DHEA) 常被用作非处方营养补充剂,在人体中代谢为雄激素和雌激素。DHEA 的不受监管使用的疗效和安全性尚不清楚。我们现在报告,DHEA 通过增加雌激素受体 (ER)-β与 Dishevelled2 (Dvl2) 的结合,诱导 AR 非反应性人前列腺癌细胞系 DU145 中的β-CTS,该细胞系为雄激素非依赖性前列腺癌 (AiPC) 细胞。这种诱导是暂时的,可通过测量 ERβ/Dvl2 结合的动力学、β-CTS 靶向基因 c-Myc 和细胞周期蛋白 D1 的蛋白表达以及细胞生长来评估。然而,在另一种人 AiPC 细胞系 PC-3 细胞中,DHEA 没有可检测到的作用,部分原因是它们的 Galpha-亚基表达较低,以及 DHEA 下调 ERβ/Dvl2 的结合。当在 PC-3 细胞中过表达 Gqα时,β-CTS 被持续诱导,包括增加 c-Myc 和细胞周期蛋白 D1 的蛋白表达。这种效应涉及到 Gqα/Dvl2 和 ERβ/Dvl2 结合的增加,并促进了细胞生长。这些活性需要 DU-145 和 PC-3 细胞中的 ERβ,因为它们被 ICI 182-780 处理失活 ERβ、小干扰 RNA 给药耗尽 ERβ或 AR 过表达阻断 ERβ所阻断。这些数据表明,激活β-CTS 的新途径在 AiPC 的进展中发挥作用。尽管 DHEA 可能通过雄激素或雌激素途径增强 PrCa 细胞的生长,但 DHEA 给药对临床前列腺功能的影响仍有待确定。