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Updated: Feb 22, 2026
Dual Bioluminescence Imaging of Tumor Progression and Angiogenesis
Published on: August 1, 2019
PLK1-Targeted Fluorescent Tumor Imaging with High Signal-to-Background Ratio
Ji-Ting Hou1, Kyung-Phil Ko, Hu Shi2
1Hubei Collaborative Innovation Center for Biomass Conversion and Utilization, Hubei Engineering University , Xiaogan 432000, China.
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.
Insights
Researchers developed novel fluorescent probes to visualize cancer cells and tumors by targeting polo-like kinase 1 (PLK1). These probes enable precise imaging of PLK1-expressing tumors, offering new diagnostic and therapeutic strategies.
Area of Science:
- Biomedical Imaging
- Molecular Biology
- Oncology
Background:
- Polo-like kinase 1 (PLK1) is crucial for cell division and a potential cancer therapeutic target.
- Targeted imaging agents are needed for precise cancer diagnosis and therapy.
Purpose of the Study:
- To develop and evaluate small molecular fluorescent probes for PLK1-targeted imaging.
- To investigate the potential of these probes for visualizing PLK1-expressing cancer cells and tumors.
Main Methods:
- Synthesis of two novel fluorescent probes (1 and 2) conjugated to a PLK1 inhibitor (SBE13).
- Computational studies: enzymatic docking and molecular dynamics simulations.
- In vitro and in vivo imaging experiments in cancer cells and tumors.
Main Results:
- Probes 1 and 2 selectively targeted and visualized PLK1-expressing cells.
- Probe 2 successfully imaged PLK1-upregulated tumors with high signal-to-background ratios.
- Demonstrated the feasibility of small-molecule based fluorescent tumor imaging using PLK1 as a target.
Conclusions:
- Developed the first small-molecule fluorescent probes for PLK1-targeted tumor imaging.
- These probes offer a promising tool for cancer diagnosis and precision therapeutics.
- Opens new avenues for visualizing and treating PLK1-driven cancers.
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