title: Strained cyclooctyne as a molecular platform for construction of multimodal imaging probes.
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.
authors: State Key Laboratory of Virology, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Ministry of Education, and Wuhan University School of Pharmaceutical Sciences, Wuhan 430071 (China); Molecular Imaging Program at Stanford (MIPS), Bio-X Program, and Department of Radiology, Stanford University, California, 94305-5344 (USA).
authors: Yao
authors: Y
authors: Sun
authors: Xiaowei
authors: X
authors: Ma
authors: Kai
authors: K
authors: Cheng
authors: Biying
authors: B
authors: Wu
authors: Jianli
authors: J
authors: Duan
authors: Hao
authors: H
authors: Chen
authors: Lihong
authors: L
authors: Bu
authors: Ruiping
authors: R
authors: Zhang
authors: Xianming
authors: X
authors: Hu
authors: Zixin
authors: Z
authors: Deng
authors: Lei
authors: L
authors: Xing
authors: Xuechuan
authors: X
authors: Hong
authors: Zhen
authors: Z
authors: Cheng
mesh_terms: D000480:Alkynes / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D045744:Cell Line, Tumor; D034242:Cyclooctanes / Q000737:chemistry* / Q000493:pharmacokinetics; D004195:Disease Models, Animal; D006801:Humans; D051379:Mice; D057054:Molecular Imaging; D015335:Molecular Probes / Q000737:chemistry* / Q000493:pharmacokinetics; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000175:diagnosis*; D049268:Positron-Emission Tomography; D013438:Sulfhydryl Compounds / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D000480:Alkynes; D034242:Cyclooctanes; D015335:Molecular Probes; D013438:Sulfhydryl Compounds
keywords: alkynes; fluorescence; imaging agents; strained molecules; thiols