PLK1-Targeted Fluorescent Tumor Imaging with High Signal-to-Background Ratio,ACS Sensors

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PLK1-Targeted Fluorescent Tumor Imaging with High Signal-to-Background Ratio
ACS Sensors ( IF 8.2 ) Pub Date : 2017-09-28 00:00:00 , DOI: 10.1021/acssensors.7b00544
Ji-Ting Hou ₁ , Kyung-Phil Ko , Hu Shi ₂ , Wen Xiu Ren , Peter Verwilst , Seyoung Koo , Jin Yong Lee ₂ , Sung-Gil Chi , Jong Seung Kim

Affiliation

As significantly expressed during cell division, polo-like kinase 1 (PLK1) plays crucial roles in numerous mitotic events and has attracted interest as a potential therapeutic marker in oncological drug discovery. We prepared two small molecular fluorescent probes, 1 and 2, conjugated to SBE13 (a type II PLK1 inhibitor) to investigate the PLK1-targeted imaging of cancer cells and tumors. Enzymatic docking studies, molecular dynamics simulations, and in vitro and in vivo imaging experiments all supported the selective targeting and visualization of PLK1 expressing cells by probes 1 and 2, and probe 2 was successfully demonstrated to image PLK1-upregulated tumors with remarkable signal-to-background ratios. These findings represent the first example of small-molecule based fluorescent imaging of tumors using PLK1 as a target, which could provide new avenues for tumor diagnosis and precision therapeutics.

中文翻译：

具有高信噪比的PLK1靶向荧光肿瘤成像

正如在细胞分裂过程中明显表达的那样，polo样激酶1（PLK1）在许多有丝分裂事件中都起着至关重要的作用，并作为肿瘤药物发现中的潜在治疗标记物引起了人们的兴趣。我们准备了两种与SBE13（II型PLK1抑制剂）偶联的小分子荧光探针1和2，以研究靶向PLK1的癌细胞和肿瘤成像。酶对接研究，分子动力学模拟以及体外和体内成像实验均支持探针1和2以及探针2对PLK1表达细胞的选择性靶向和可视化已成功证明可对PLK1上调的肿瘤成像，并具有显着的信噪比。这些发现代表了使用PLK1作为靶标的基于小分子的肿瘤荧光成像的第一个实例，这可以为肿瘤诊断和精确治疗提供新途径。

更新日期：2017-09-28

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