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Strained Cyclooctyne as a Molecular Platform for Construction of Multimodal Imaging Probes
Author(s) -
Sun Yao,
Ma Xiaowei,
Cheng Kai,
Wu Biying,
Duan Jianli,
Chen Hao,
Bu Lihong,
Zhang Ruiping,
Hu Xianming,
Deng Zixin,
Xing Lei,
Hong Xuechuan,
Cheng Zhen
Publication year - 2015
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201500941
Subject(s) - molecular imaging , clinical imaging , imaging agent , pet imaging , biomedical engineering , materials science , nanotechnology , chemistry , positron emission tomography , nuclear medicine , medicine , radiology , biology , in vivo , microbiology and biotechnology
Abstract 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: 64 Cu‐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 64 Cu‐CHS1 a promising probe for clinical use.