PLK1-Targeted Fluorescent Tumor Imaging with High Signal-to-Background Ratio
- Authors
- Hou, Ji-Ting; Ko, Kyung-Phil; Shi, Hu; Ren, Wen Xiu; Verwilst, Peter; Koo, Seyoung; Lee, Jin Yong; Chi, Sung-Gil; Kim, Jong Seung
- Issue Date
- 10월-2017
- Publisher
- AMER CHEMICAL SOC
- Keywords
- PLK1; SBE13; targeted imaging; high SBR ratio; fluorescence
- Citation
- ACS SENSORS, v.2, no.10, pp.1512 - 1516
- Indexed
- SCIE
SCOPUS
- Journal Title
- ACS SENSORS
- Volume
- 2
- Number
- 10
- Start Page
- 1512
- End Page
- 1516
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/82086
- DOI
- 10.1021/acssensors.7b00544
- ISSN
- 2379-3694
- Abstract
- 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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- Appears in
Collections - Graduate School > Department of Life Sciences > 1. Journal Articles
- College of Science > Department of Chemistry > 1. Journal Articles
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