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

doi:10.1021/acssensors.7b00544

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 journal › Article › peer-review

20 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 language	English
Pages (from-to)	1512-1516
Number of pages	5
Journal	ACS Sensors
Volume	2
Issue number	10
DOIs	https://doi.org/10.1021/acssensors.7b00544
Publication status	Published - 2017 Oct 27

Bibliographical note

Funding Information:
This work was supported by the Ministry of Science, ICT & Future Planning (MSIP) of Korea (No. 2009-0081566 for J.S.K.) National Research Foundation of Korea (NRF-20158A2A1A01005389 for S.G.C.).

Keywords

PLK1
SBE13
fluorescence
high SBR ratio
targeted imaging

ASJC Scopus subject areas

Bioengineering
Instrumentation
Process Chemistry and Technology
Fluid Flow and Transfer Processes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1021/acssensors.7b00544

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title = "PLK1-Targeted Fluorescent Tumor Imaging with High Signal-to-Background Ratio",

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.",

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note = "Funding Information: This work was supported by the Ministry of Science, ICT & Future Planning (MSIP) of Korea (No. 2009-0081566 for J.S.K.) National Research Foundation of Korea (NRF-20158A2A1A01005389 for S.G.C.).",

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AU - Ren, Wen Xiu

AU - Verwilst, Peter

AU - Koo, Seyoung

AU - Lee, Jin Yong

AU - Chi, Sung-Gil

AU - Kim, Jong Seung

N1 - Funding Information: This work was supported by the Ministry of Science, ICT & Future Planning (MSIP) of Korea (No. 2009-0081566 for J.S.K.) National Research Foundation of Korea (NRF-20158A2A1A01005389 for S.G.C.).

PY - 2017/10/27

Y1 - 2017/10/27

N2 - 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.

AB - 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.

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

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

UN SDGs

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