Strained Cyclooctyne as a Molecular Platform for Construction of Multimodal Imaging Probes
Strained Cyclooctyne as a Molecular Platform for Construction of Multimodal Imaging Probes
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DOI：
10.1002/anie.201500941
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发表时间：
2015-05-11
影响因子：
16.6
通讯作者：
Cheng, Zhen
中科院分区：
文献类型：
--
作者：
Sun, Yao;Ma, Xiaowei;Cheng, Zhen
基于小分子的多模态和多功能成像探针在生物医学研究中发挥着突出的作用，并具有很高的临床翻译能力。本研究建立了一种新的多模态成像平台，该平台使用碱催化的硫醇双加成到应变内部炔如双环[6.1.0]壬炔上，从而允许以无保护基的方式高度选择性地组装各种功能单元。利用该分子平台，制备了新型双模态（PET和NIRF）uPAR靶向成像探针Cu-64-CHS 1，并在U87 MG细胞和荷瘤小鼠模型中进行了评价。在小动物模型中实现了优异的PET/NIRF成像特征，例如良好的肿瘤摄取（注射后2小时为3.69%ID/g）、高肿瘤对比度和特异性。这些有吸引力的成像特性使Cu-64-CHS 1成为一种有前途的临床应用探针。
Small-molecule-based multimodal and multifunctional imaging probes play prominent roles in biomedical research and have high clinical translation ability. A novel multimodal imaging platform using base-catalyzed double addition of thiols to a strained internal alkyne such as bicyclo[6.1.0] nonyne has been established in this study, thus allowing highly selective assembly of various functional units in a protecting-group-free manner. Using this molecular platform, novel dual-modality (PET and NIRF) uPAR-targeted imaging probe: Cu-64-CHS1 was prepared and evaluated in U87MG cells and tumor-bearing mice models. The excellent PET/NIRF imaging characteristics such as good tumor uptake (3.69% ID/g at 2 h post-injection), high tumor contrast, and specificity were achieved in the small-animal models. These attractive imaging properties make Cu-64-CHS1 a promising probe for clinical use.