Strained Cyclooctyne as a Molecular Platform for Construction of Multimodal Imaging Probes1. (20th March 2015)

• Record Type: Journal Article
• Authors: 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
• Is Part Of: Angewandte Chemie. Volume 127:Number 20(2015)
• Page Start: 6079
• Page End: 6082
• Publication Date: 2015-03-20
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1002/ange.201500941
• Languages: English
• ISSNs: 0044-8249

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <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: ⁶⁴Cu‐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 ⁶⁴Cu‐CHS1 a promising probe for clinical use.</p> </abstract>