期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 54, 期 20, 页码 5981-5984出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201500941
关键词
alkynes; fluorescence; imaging agents; strained molecules; thiols
资金
- Office of Science (BER), U.S. Department of Energy [DE-SC0008397]
- NIH In vivo Cellular Molecular Imaging Center (ICMIC) [P50 CA114747]
- NSFC [81373254, 81301268, 21390402]
- NSFHP [2014CFB704]
- International S&T Cooperation Program of China [2015DFA30440, 2014DFB30020]
- Key Project of Chinese Ministry of Education [313040]
- Ministry of Education of China [5052012306001]
- China Scholarship Council Fellowship
- Fundamental Research Funds for the Central Universities
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.
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