Department of Biochemistry, Medical College of Wisconsin, Milwaukee, WI 53226, USA.
Cancer Lett. 2013 Oct 1;339(1):144-51. doi: 10.1016/j.canlet.2013.07.006. Epub 2013 Jul 12.
Medullary thyroid carcinoma (MTC) is a neoplasm of the endocrine system, which originates from parafollicular C-cells of the thyroid gland. For MTC therapy, the Food and Drug Administration recently approved vandetanib and cabozantinib, multi-kinase inhibitors targeting RET and other tyrosine kinase receptors of vascular endothelial growth factor, epidermal growth factor, or hepatocyte growth factor. Nevertheless, not all patients with the progressive MTC respond to these drugs, requiring the development of additional therapeutic modalities that have distinct activity. Previously, we reported that expression of activated Ras or Raf in the human MTC cell lines, TT and MZ-CRC-1, can induce growth arrest and RET downregulation via a leukemia inhibitory factor (LIF)-mediated autocrine/paracrine loop. In this study, we aimed to evaluate bacterially-produced recombinant human LIF for its efficacy to suppress human MTC xenografts in mice. Here, we report that, consistent with its effects in vitro, locally or systemically administered recombinant LIF effectively suppressed growth of TT and MZ-CRC-1 xenografts in mice. Further, as predicted from its effects in TT and MZ-CRC-1 cell cultures in vitro, recombinant LIF activated the JAK/STAT pathway and downregulated RET and E2F1 expression in tumors in mice. These results suggest that LIF is a potent cytostatic agent for MTC cells, which regulates unique mechanisms that are not targeted by currently available therapeutic agents.
甲状腺髓样癌 (MTC) 是一种内分泌系统肿瘤,起源于甲状腺滤泡旁 C 细胞。为了治疗 MTC,美国食品和药物管理局最近批准了凡德他尼和卡博替尼,这两种多激酶抑制剂靶向 RET 和血管内皮生长因子、表皮生长因子或肝细胞生长因子的其他酪氨酸激酶受体。然而,并非所有进展性 MTC 患者对这些药物都有反应,需要开发具有不同活性的其他治疗方式。先前,我们报道在人 MTC 细胞系 TT 和 MZ-CRC-1 中表达激活的 Ras 或 Raf 可以通过白血病抑制因子 (LIF) 介导的自分泌/旁分泌环诱导生长停滞和 RET 下调。在这项研究中,我们旨在评估细菌产生的重组人 LIF 对抑制小鼠人 MTC 异种移植物的疗效。在这里,我们报告说,与体外的作用一致,局部或系统给予重组 LIF 可有效抑制 TT 和 MZ-CRC-1 异种移植物在小鼠中的生长。此外,正如体外 TT 和 MZ-CRC-1 细胞培养物中的作用所预测的那样,重组 LIF 激活了 JAK/STAT 途径,并下调了小鼠肿瘤中的 RET 和 E2F1 表达。这些结果表明 LIF 是 MTC 细胞的一种有效的细胞生长抑制剂,它调节了目前可用治疗药物无法靶向的独特机制。