Julius L. Chambers Biomedical/Biotechnology Research Institute, Department of Biological and Biomedical Sciences, North Carolina Central University, North Carolina Research Campus, Kannapolis, North Carolina, United States of America.
Basic Medical College of Zhengzhou University, Zhengzhou, Henan, P.R. China.
PLoS One. 2019 May 6;14(5):e0216469. doi: 10.1371/journal.pone.0216469. eCollection 2019.
Exposure to bisphenol A (BPA), an endocrine-disrupting compound, is associated with increased risk of estrogen-related diseases, including estrogen receptor-positive (ER+) breast cancer. Although bisphenol analogs, i.e. bisphenol AF (BPAF), have replaced BPA in industrial settings, increasing data indicate that these alternatives may have similar or even more potent estrogenic effects. As such, BPAF exhibits increased ER binding affinities than BPA in biochemical assays. However, preclinical studies exploring the effects of BPAF on ER+ breast cancer are missing mechanistic data. Thus, we aimed to characterize the effects of BPAF on MCF-7 and T47D ER+ breast cancer cells with mechanistic insight. We found that BPAF promoted cell growth and cell cycle progression concurrently with BPAF-induced ERα transcriptional activity and ER-RTK signaling activation. ER signaling blockage revealed that BPAF-induced cell proliferation and ER-RTK crosstalk were ER-dependent. Gene expression data demonstrated that AREG is a sensitive target of BPAF in our in vitro models. Importantly, we determined that AREG upregulation is necessary for BPAF-induced cellular responses. Ultimately, our novel finding that AREG mediates BPAF-induced ER-RTK crosstalk in ER+ breast cancer cells supports future studies to characterize the impact of BPAF on human ER+ breast cancer risk and to assess the safety profile of BPAF.
双酚 A(BPA)是一种内分泌干扰化合物,接触 BPA 会增加与雌激素相关的疾病的风险,包括雌激素受体阳性(ER+)乳腺癌。尽管双酚类似物,如双酚 AF(BPAF),已在工业环境中取代 BPA,但越来越多的数据表明这些替代品可能具有类似甚至更强的雌激素作用。因此,BPAF 在生化测定中比 BPA 具有更高的 ER 结合亲和力。然而,探索 BPAF 对 ER+乳腺癌影响的临床前研究缺乏机制数据。因此,我们旨在通过深入的机制研究来表征 BPAF 对 MCF-7 和 T47D ER+乳腺癌细胞的影响。我们发现 BPAF 可促进细胞生长和细胞周期进程,同时诱导 ERα转录活性和 ER-RTK 信号激活。ER 信号阻断揭示 BPAF 诱导的细胞增殖和 ER-RTK 串扰依赖于 ER。基因表达数据表明,AREG 是我们体外模型中 BPAF 的敏感靶标。重要的是,我们确定 AREG 的上调是 BPAF 诱导细胞反应所必需的。最终,我们的新发现表明,AREG 介导了 BPAF 诱导的 ER+乳腺癌细胞中的 ER-RTK 串扰,这支持了未来研究 BPAF 对人类 ER+乳腺癌风险的影响以及评估 BPAF 安全性概况的研究。