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当代肿瘤药物靶点

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ISSN (Print): 1568-0096
ISSN (Online): 1873-5576

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Research Article

碘化钠共转运蛋白刺激后诱导MCF-7乳腺癌细胞中[18F]四氟硼酸盐的摄取。

卷 20, 期 2, 2020

页: [146 - 155] 页: 10

弟呕挨: 10.2174/1568009619666191016145602

价格: $65

摘要

背景：人类碘化钠共转运蛋白（hNIS）已成为核医学中与甲状腺相关疾病的最重要靶标。尽管还可以在甲状腺外肿瘤中确定hNIS的表达，但尚未在临床上利用正电子发射断层显像对hNIS进行成像。目的：在这里，我们评估了改良的放射合成和药理学刺激后，内源性表达hNIS的乳腺癌细胞系MCF-7中新型hNIS底物[18F]四氟硼酸盐（[18F] TFB）的积累。 方法：在温和的反应条件下（40°C，25分钟）制备[18F] TFB，并在全反式维甲酸和美沙酮衍生物联合预处理的MCF-7细胞中研究其吸收特性，并将其与临床比较确定了示踪剂[131I]碘化物和[99mTc]高tech酸盐。示踪剂积累的特异性通过使用NaBF4，KSO3F，KI和KIO3的抑制实验进行评估。 结果：[18F] TFB在高压液相色谱分离后40分钟内以24.0} 6.6％（n = 17）的放射化学产率获得，而在适应后45分钟内以26.8} 6.2％（n = 13）的放射化学产率得到。使用较高启动活动（> 10 GBq）的综合模块上的过程。药理处理后，与对照实验相比，MCF-7细胞表面hNIS的表达增加了4倍，导致[18F] TFB摄入细胞明显更高（最多58倍）。使用各种NIS底物的抑制研究证实了[18F] TFB对hNIS的特异性。 结论：在人类模型中，[18F] TFB被证明是一种有前途的hNIS底物，可通过人类MCF-7乳腺癌细胞系对异种移植研究和患者进行体内评估。

关键词: 碘化钠共转运蛋白（NIS），[18F]四氟硼酸盐，[18F] TFB，乳腺癌，MCF-7，PET成像。

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