Molecular Biology Graduate Program, Department of Pathology, University of Colorado Anschutz Medical Campus, Aurora, CO, USA.
Molecular Biology Graduate Program, Department of Biochemistry and Molecular Genetics, University of Colorado School of Medicine, Aurora, CO, USA.
Endocrinology. 2021 Feb 1;162(2). doi: 10.1210/endocr/bqaa226.
Triple-negative breast cancer (TNBC) is an aggressive subtype with peak recurrence as metastatic disease within the first few years of diagnosis. Androgen receptor (AR) expression is increased in anchorage-independent cells in TNBC preclinical models. Both AR knockdown and inhibition lead to reduced TNBC invasion in vitro, reduced tumorigenicity, and less recurrence in vivo in preclinical models. Transforming growth factor β (TGFβ) pathway gene signatures also increased during anchorage-independent survival both in vitro and in vivo in preclinical models and in circulating tumor cells (CTCs) from patients during emergence of chemo resistant disease. We hypothesized that a positive loop between AR and TGFβ signaling facilitates TNBC anchorage-independent survival. We find that multiple components of the TGFβ pathway, including TGFβ1 and 3, as well as pathway activity measured by nuclear localization and transcriptional activity of phosphorylated Smad3, are enhanced in anchorage-independent conditions. Further, exogenous TGFβ increased AR protein while TGFβ inhibition decreased AR and TNBC viability, particularly under anchorage-independent culture conditions. ChIP-seq experiments revealed AR binding to TGFB1 and SMAD3 regulatory regions in MDA-MB-453 cells. In clinical datasets, TGFB3 and AR positively correlate and high expression of both genes together corresponded to significantly worse recurrence-free and overall survival in both ER-negative and basal-like breast cancer. Finally, inhibiting both AR and TGFβ decreased cell survival, particularly under anchorage-independent conditions. These findings warrant further investigations into whether combined inhibition of AR and TGFβ pathways might decrease metastatic recurrence rates and mortality from TNBC.
三阴性乳腺癌(TNBC)是一种侵袭性亚型,在诊断后的最初几年内,复发高峰为转移性疾病。雄激素受体(AR)在 TNBC 临床前模型中的无锚定依赖性细胞中表达增加。AR 敲低和抑制均可导致 TNBC 体外侵袭减少、肿瘤发生减少以及临床前模型中体内复发减少。转化生长因子 β(TGFβ)通路基因特征也在临床前模型中的无锚定依赖性存活以及患者循环肿瘤细胞(CTC)中增加,这些 CTC 是在出现化疗耐药性疾病时出现的。我们假设 AR 和 TGFβ 信号之间的正反馈环路促进了 TNBC 的无锚定依赖性存活。我们发现 TGFβ 通路的多个成分,包括 TGFβ1 和 3,以及通过核定位和磷酸化 Smad3 的转录活性测量的通路活性,在无锚定条件下增强。此外,外源性 TGFβ增加了 AR 蛋白,而 TGFβ 抑制减少了 AR 和 TNBC 的活力,特别是在无锚定依赖性培养条件下。ChIP-seq 实验显示 AR 与 MDA-MB-453 细胞中的 TGFB1 和 SMAD3 调节区域结合。在临床数据集,TGFB3 和 AR 呈正相关,并且这两个基因的高表达与 ER 阴性和基底样乳腺癌的无复发生存和总生存显著更差相关。最后,抑制 AR 和 TGFβ 均可降低细胞存活率,特别是在无锚定依赖性条件下。这些发现证明,进一步研究联合抑制 AR 和 TGFβ 通路是否可能降低 TNBC 的转移复发率和死亡率是合理的。