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

Ji Ting Hou, Kyung Phil Ko, Hu Shi, Wen Xiu Ren, Peter Verwilst, Seyoung Koo, Jin Yong Lee, Sung-Gil Chi, Jong Seung Kim

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1512-1516
Number of pages5
JournalACS Sensors
Volume2
Issue number10
DOIs
Publication statusPublished - 2017 Oct 27

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Keywords

  • fluorescence
  • high SBR ratio
  • PLK1
  • SBE13
  • targeted imaging

ASJC Scopus subject areas

  • Bioengineering
  • Fluid Flow and Transfer Processes
  • Process Chemistry and Technology
  • Instrumentation

Cite this

Hou, J. T., Ko, K. P., Shi, H., Ren, W. X., Verwilst, P., Koo, S., Lee, J. Y., Chi, S-G., & Kim, J. S. (2017). PLK1-Targeted Fluorescent Tumor Imaging with High Signal-to-Background Ratio. ACS Sensors, 2(10), 1512-1516. https://doi.org/10.1021/acssensors.7b00544