Strained Cyclooctyne as a Molecular Platform for Construction of Multimodal Imaging Probes

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<jats:title>Abstract</jats:title><jats:p>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: <jats:sup>64</jats:sup>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 <jats:sup>64</jats:sup>Cu‐CHS1 a promising probe for clinical use.</jats:p>

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