2-Nitroimidazole-Tricarbocyanine Conjugate as a Near-Infrared Fluorescent Probe for in Vivo Imaging of Tumor Hypoxia

被引：157

作者：

Okuda, Kensuke ^{[1
]}

Okabe, Yasuyuki ^{[1
]}

Kadonosono, Tetsuya ^{[2
]}

Ueno, Takahiro ^{[1
]}

Youssif, Bahaa G. M. ^{[1
]}

Kizaka-Kondoh, Shinae ^{[2
]}

Nagasawa, Hideko ^{[1
]}

机构：

[1] Gifu Pharmaceut Univ, Lab Pharmaceut & Med Chem, Gifu 5011196, Japan

[2] Tokyo Inst Technol, Grad Sch Biosci & Biotechnol, Dept Biomol Engn, Yokohama, Kanagawa 2268501, Japan

来源：

BIOCONJUGATE CHEMISTRY | 2012年 / 23卷 / 03期

基金：

日本学术振兴会;

关键词：

SOLID TUMORS; BINDING; CANCER; PIMONIDAZOLE; REGIONS;

D O I：

10.1021/bc2004704

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

We developed a novel near-infrared (NIR) fluorescent probe, GPU-167, for in vivo imaging of tumor hypcoda. GPU-167 comprises a tricarbocyanine dye as an NIR fluorophore and two 2-nitroimidazole moieties as exogenous hypoxia markers that undergo bioreductive activation and then selective entrapment in hypoxic cells. After treatment with GPU-167, tumor cells contained significantly higher levels of fluorescence in hypoxia than in normoxia. In vivo fluorescence imaging specifically detected GPU-167 in tumors 24 h after administration. Ex vivo analysis revealed that fluorescence showed a strong correlation with hypoxia inducible factor (HIF)-1 active hypoxic regions. These data suggest that GPU-167 is a promising in vivo optical imaging probe for tumor hypoxia.

引用

页码：324 / 329

页数：6

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