Vanderbilt University Institute of Imaging Science, Vanderbilt University Medical Center, Nashville, TN, USA.
Mol Imaging Biol. 2010 Jun;12(3):349-58. doi: 10.1007/s11307-009-0270-8. Epub 2009 Dec 1.
To quantitatively evaluate the utility of a translocator protein (TSPO)-targeted near-infrared (NIR) probe (NIR-conPK11195) for in vivo molecular imaging of TSPO in breast cancer.
NIR-conPK11195 uptake and TSPO-specificity were validated in TSPO-expressing human breast adenocarcinoma cells (MDA-MB-231). In vivo NIR-conPK11195 biodistribution and accumulation were quantitatively evaluated in athymic nude mice bearing MDA-MB-231 xenografts.
Fluorescence micrographs illustrated intracellular labeling of MDA-MB-231 cells by NIR-conPK11195. Quantitative uptake and competition assays demonstrated dose-dependent (p < 0.001) and TSPO-specific (p < 0.001) NIR-conPK11195 uptake. In vivo, NIR-conPK11195 preferentially labeled MDA-MB-231 tumors with an 11-fold (p < 0.001) and 7-fold (p < 0.001) contrast enhancement over normal tissue and unconjugated NIR dye, respectively.
NIR-conPK11195 appears to be a promising TSPO-targeted molecular imaging agent for visualization and quantification of breast cancer cells in vivo. This research represents the first study to demonstrate the feasibility of TSPO imaging as an alternative breast cancer imaging approach.
定量评估转位蛋白（TSPO）靶向近红外（NIR）探针（NIR-conPK11195）在乳腺癌体内 TSPO 分子成像中的应用。
在表达 TSPO 的人乳腺癌腺癌细胞（MDA-MB-231）中验证 NIR-conPK11195 的摄取和 TSPO 特异性。在荷 MDA-MB-231 异种移植瘤的裸鼠体内定量评估 NIR-conPK11195 的体内 NIR-conPK11195 生物分布和积累。
荧光显微镜图显示 NIR-conPK11195 对 MDA-MB-231 细胞的细胞内标记。定量摄取和竞争实验表明，NIR-conPK11195 的摄取呈剂量依赖性（p < 0.001）和 TSPO 特异性（p < 0.001）。在体内，NIR-conPK11195 优先标记 MDA-MB-231 肿瘤，与正常组织相比，对比度增强了 11 倍（p < 0.001），与未结合的 NIR 染料相比，对比度增强了 7 倍（p < 0.001）。
NIR-conPK11195 似乎是一种有前途的 TSPO 靶向分子成像剂，可用于可视化和定量体内乳腺癌细胞。这项研究代表了首次证明 TSPO 成像作为替代乳腺癌成像方法的可行性的研究。
