An optical probe for noninvasive molecular imaging of orthotopic brain tumors overexpressing epidermal growth factor receptor.
An optical probe for noninvasive molecular imaging of orthotopic brain tumors overexpressing epidermal growth factor receptor.
复制标题
DOI：
10.1158/1535-7163.mct-12-0211
复制
发表时间：
2012-10
影响因子：
5.7
通讯作者：
Basilion JP
中科院分区：
文献类型：
--
作者：
Agnes RS;Broome AM;Wang J;Verma A;Lavik K;Basilion JP
我们已经开发了一种近红外（NIR）探针，该探针靶向过表达EGF受体（EGFR）的细胞，用于对活体脑胶质母细胞瘤进行成像。用不同长度的单离散聚乙二醇（PEG）单元和近红外Cy5.5荧光染料修饰EGFR特异性肽。先导化合物化合物2在体外表达EGFR的胶质母细胞瘤细胞中表现出良好的结合（8.9 μmol/L）和细胞摄取。体内研究表明，该探针能够选择性地标记胶质母细胞瘤来源的原位脑肿瘤。利用荧光介导的分子断层扫描技术对肽与肿瘤结合的体内图像进行分析，发现该化合物可以区分表达不同水平EGFR的肿瘤。本文提供的数据首次展示了通过使用分子成像装置的靶向近红外荧光探针在活体动物中表达EGFR的肿瘤的差异定量。
We have developed a near-infrared (NIR) probe that targets cells overexpressing the EGF receptor (EGFR) for imaging glioblastoma brain tumors in live subjects. A peptide specific for the EGFR was modified with various lengths of monodiscrete polyethylene glycol (PEG) units and a NIR Cy5.5 fluorescence dye. The lead compound, compound 2, with one unit of PEG displayed good binding (8.9 μmol/L) and cellular uptake in glioblastoma cells overexpressing EGFR in vitro. The in vivo studies have shown that the probe was able to selectively label glioblastoma-derived orthotopic brain tumors. In vivo image analyses of peptide binding to the tumors using fluorescence-mediated molecular tomography revealed that the compound could distinguish between tumors expressing different levels of EGFR. The data presented here represent the first demonstration of differential quantitation of tumors expressing EGFR in live animals by a targeted NIR fluorescence probe using a molecular imaging device.