In Vivo Gastric Cancer Targeting and Imaging Using Novel Symmetric Cyanine Dye-Conjugated GX1 Peptide Probes
In Vivo Gastric Cancer Targeting and Imaging Using Novel Symmetric Cyanine Dye-Conjugated GX1 Peptide Probes
复制标题
使用新型对称花青染料缀合 GX1 肽探针进行体内胃癌靶向和成像
DOI：
10.1021/bc3006539
复制
发表时间：
2013-07-01
影响因子：
4.7
通讯作者：
Tian, Jie
中科院分区：
文献类型：
--
作者：
Xin, Jing;Zhang, Xianghan;Tian, Jie
为了促进癌症荧光成像转化为临床实践，需要开发稳定且高度特异性和灵敏度低毒性的靶向荧光探针。GX 1是一种胃肿瘤血管生成标记物候选物，有望用于体内早期胃癌检测的分子成像探针的靶向特异性递送。在这项研究中，我们描述了使用对称合成方法设计和合成一系列新型五次甲基花青染料，并进一步将这些染料与GX 1偶联，使其与胃癌血管特异性结合。这种有效的合成路线可以减少不需要的副产物，同时提高产率。此外，体内荧光成像显示，这种新型靶向探针选择性地在SGC-7901皮下异种移植模型的肿瘤部位积累。这种新型的血管靶向分子探针与荧光成像技术的结合可能会提高胃癌的早期检测，转移检测和抗肿瘤血管生成治疗。
To facilitate the translation of cancer fluorescence imaging into clinical practice, the development of stable and highly specific and sensitive targeted fluorescence probes with low toxicity is desirable. GX1, a gastric tumor angiogenesis marker candidate, holds promise in the target-specific delivery of molecular imaging probes for early gastric cancer detection in vivo. In this study, we describe the design and synthesis of a series of novel penta-methine cyanine dyes using the symmetric synthesis method and further conjugated the dyes with GX1, allowing specific binding to the vasculature of gastric cancer. This efficient synthetic route can decrease the undesired byproducts, while increasing yield. Furthermore, in vivo fluorescence imaging revealed that this novel targeted probe accumulates selectively in the tumor site of SGC-7901 subcutaneous xenograft models. The combination of such novel vasculature-targeted molecular probes with fluorescence imaging technology may improve early detection, metastasis detection, and antitumor angiogenesis therapy for gastric cancer.