期刊
ACS SENSORS
卷 2, 期 10, 页码 1512-1516出版社
AMER CHEMICAL SOC
DOI: 10.1021/acssensors.7b00544
关键词
PLK1; SBE13; targeted imaging; high SBR ratio; fluorescence
资金
- Ministry of Science, ICT & Future Planning (MSIP) of Korea [2009-0081566]
- National Research Foundation of Korea [NRF-20158A2A1A01005389]
As significantly expressed during cell division, polo-like kinase 1 (PLKl) 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 PLKl as a target, which could provide new avenues for tumor diagnosis and precision therapeutics.
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