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

被引：19

作者：

Hou, Ji-Ting ^{[1
,4
]}

Ko, Kyung-Phil ^{[2
]}

Shi, Hu ^{[3
]}

Ren, Wen Xiu ^{[1
]}

Verwilst, Peter ^{[1
]}

Koo, Seyoung ^{[1
]}

Lee, Jin Yong ^{[3
]}

Chi, Sung-Gil ^{[2
]}

Kim, Jong Seung ^{[1
]}

机构：

[1] Korea Univ, Dept Chem, Seoul 02841, South Korea

[2] Korea Univ, Dept Life Sci, Seoul 02841, South Korea

[3] Sungkyunkwan Univ, Dept Chem, Suwon 16419, South Korea

[4] Hube Engn Univ, Hube Collaborat Innovat Ctr Biomass Convers & Util, Xiaogan 432000, Peoples R China

来源：

ACS SENSORS | 2017年 / 2卷 / 10期

基金：

新加坡国家研究基金会;

关键词：

PLK1; SBE13; targeted imaging; high SBR ratio; fluorescence; KINASE; 1; CANCER THERAPEUTICS; IN-VIVO; POLO; PLK1; AGENTS; DESIGN; PRINCIPLES; THERAPY; PEPTIDE;

D O I：

10.1021/acssensors.7b00544

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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.

引用

页码：1512 / 1516

页数：5

共 31 条

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