Serviço de Endocrinologia, Diabetes e Metabolismo do CHULN-Hospital Santa Maria, Lisboa, Portugal.
BioISI-Biosystems and Integrative Sciences Institute, Faculdade de Ciências da Universidade de Lisboa, Lisboa, Portugal.
PLoS One. 2020 Feb 12;15(2):e0228794. doi: 10.1371/journal.pone.0228794. eCollection 2020.
The sodium-iodide symporter (NIS) mediates transport of iodide across the basolateral membrane of thyroid cells. NIS expression in thyroid cancer (TC) cells allows the use of radioactive iodine (RAI) as a diagnostic and therapeutic tool, being RAI therapy the systemic treatment of choice for metastatic disease. Still, a significant proportion of patients with advanced TC lose the ability to respond to RAI therapy and no effective alternative therapies are available. Defective NIS expression is the main reason for impaired iodide uptake in TC and NIS downregulation has been associated with several pathways linked to malignant transformation. NF-κB signaling is one of the pathways associated with TC. Interestingly, NIS expression can be negatively regulated by TNF-α, a bona fide activator of NF-κB with a central role in thyroid autoimmunity. This prompted us to clarify NF-kB's role in this process. We confirmed that TNF-α leads to downregulation of TSH-induced NIS expression in non-neoplastic thyroid follicular cell-derived models. Notably, a similar effect was observed when NF-κB activation was triggered independently of ligand-receptor specificity, using phorbol-myristate-acetate (PMA). TNF-α and PMA downregulation of NIS expression was reverted when NF-κB-dependent transcription was blocked, demonstrating the requirement for NF-kB activity. Additionally, TNF-α and PMA were shown to have a negative impact on TSH-induced iodide uptake, consistent with the observed transcriptional downregulation of NIS. Our data support the involvement of NF-κB-directed transcription in the modulation of NIS expression, where up- or down-regulation of NIS depends on the combined output to NF-κB of several converging pathways. A better understanding of the mechanisms underlying NIS expression in the context of normal thyroid physiology may guide the development of pharmacological strategies to increase the efficiency of iodide uptake. Such strategies would be extremely useful in improving the response to RAI therapy in refractory-TC.
钠碘同向转运体(NIS)介导碘离子穿过甲状腺细胞的基底外侧膜转运。甲状腺癌细胞(TC)中 NIS 的表达使放射性碘(RAI)能够作为诊断和治疗工具,RAI 治疗是转移性疾病的首选全身治疗方法。尽管如此,相当一部分晚期 TC 患者失去了对 RAI 治疗的反应能力,并且没有有效的替代治疗方法。NIS 表达缺陷是 TC 中碘摄取受损的主要原因,NIS 下调与几种与恶性转化相关的途径有关。NF-κB 信号通路是与 TC 相关的途径之一。有趣的是,TNF-α可以负向调节 NIS 的表达,TNF-α 是 NF-κB 的真正激活剂,在甲状腺自身免疫中起核心作用。这促使我们阐明 NF-κB 在这个过程中的作用。我们证实,TNF-α导致非肿瘤性甲状腺滤泡细胞衍生模型中 TSH 诱导的 NIS 表达下调。值得注意的是,当使用佛波醇肉豆蔻酸乙酸酯(PMA)独立于配体-受体特异性触发 NF-κB 激活时,观察到类似的效果。当 NF-κB 依赖性转录被阻断时,TNF-α 和 PMA 下调 NIS 表达被逆转,表明 NF-kB 活性的必要性。此外,TNF-α 和 PMA 对 TSH 诱导的碘摄取有负面影响,与观察到的 NIS 转录下调一致。我们的数据支持 NF-κB 定向转录参与 NIS 表达的调节,其中 NIS 的上调或下调取决于几个汇聚途径对 NF-κB 的综合输出。更好地了解正常甲状腺生理学中 NIS 表达的机制可能有助于开发提高碘摄取效率的药物策略。在难治性 TC 中,这些策略对于提高对 RAI 治疗的反应非常有用。