Department of Cancer Biology, Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, PA 19107, USA.
Am J Pathol. 2010 Dec;177(6):2971-83. doi: 10.2353/ajpath.2010.090399. Epub 2010 Oct 15.
Basal levels of nuclear localized, tyrosine phosphorylated Stat5 are present in healthy human breast epithelia. In contrast, Stat5 phosphorylation is frequently lost during breast cancer progression, a finding that correlates with loss of histological differentiation and poor patient prognosis. Identifying the mechanisms underlying loss of Stat5 phosphorylation could provide novel targets for breast cancer therapy. Pervanadate, a general tyrosine phosphatase inhibitor, revealed marked phosphatase regulation of Stat5 activity in breast cancer cells. Lentiviral-mediated shRNA allowed specific examination of the regulatory role of five tyrosine phosphatases (PTP1B, TC-PTP, SHP1, SHP2, and VHR), previously implicated in Stat5 regulation in various systems. Enhanced and sustained prolactin-induced Stat5 tyrosine phosphorylation was observed in T47D and MCF7 breast cancer cells selectively in response to PTP1B depletion. Conversely, PTP1B overexpression suppressed prolactin-induced Stat5 tyrosine phosphorylation. Furthermore, PTP1B knockdown increased Stat5 reporter gene activity. Mechanistically, PTP1B suppression of Stat5 phosphorylation was mediated, at least in part, through inhibitory dephosphorylation of the Stat5 tyrosine kinase, Jak2. PTP1B knockdown enhanced sensitivity of T47D cells to prolactin phosphorylation of Stat5 by reducing the EC(50) from 7.2 nmol/L to 2.5 nmol/L. Immunohistochemical analyses of two independent clinical breast cancer materials revealed significant negative correlations between levels of active Stat5 and PTP1B, but not TC-PTP. Collectively, our data implicate PTP1B as an important negative regulator of Stat5 phosphorylation in invasive breast cancer.
在健康的人乳腺上皮细胞中存在核定位的酪氨酸磷酸化 Stat5 的基础水平。相比之下,Stat5 的磷酸化在乳腺癌进展过程中经常丢失,这一发现与组织学分化的丧失和患者预后不良相关。确定导致 Stat5 磷酸化丢失的机制可能为乳腺癌治疗提供新的靶点。过钒酸钠是一种通用的酪氨酸磷酸酶抑制剂,它揭示了 Stat5 活性在乳腺癌细胞中受到明显的磷酸酶调节。慢病毒介导的 shRNA 允许特异性检查五种酪氨酸磷酸酶(PTP1B、TC-PTP、SHP1、SHP2 和 VHR)的调节作用,这些酶以前在各种系统中被认为与 Stat5 的调节有关。在 T47D 和 MCF7 乳腺癌细胞中,观察到增强和持续的催乳素诱导的 Stat5 酪氨酸磷酸化,这是对 PTP1B 消耗的选择性反应。相反,PTP1B 的过表达抑制了催乳素诱导的 Stat5 酪氨酸磷酸化。此外,PTP1B 的敲低增加了 Stat5 报告基因的活性。从机制上讲,PTP1B 对 Stat5 磷酸化的抑制至少部分是通过 Jak2 的抑制性去磷酸化介导的。PTP1B 的敲低通过将 T47D 细胞对 Stat5 的催乳素磷酸化的 EC(50)从 7.2 nmol/L 降低到 2.5 nmol/L,从而增强了对 T47D 细胞的敏感性。对两份独立的临床乳腺癌材料的免疫组织化学分析显示,活性 Stat5 和 PTP1B 之间存在显著的负相关,但与 TC-PTP 无关。总之,我们的数据表明 PTP1B 是侵袭性乳腺癌中 Stat5 磷酸化的重要负调节因子。