期刊
JOURNAL OF FLUORINE CHEMISTRY
卷 174, 期 -, 页码 142-147出版社
ELSEVIER SCIENCE SA
DOI: 10.1016/j.jfluchem.2014.11.009
关键词
F-18-labeling; Copper-free click chemistry; Fluorine-18; Pretargeting; PET imaging; Radiotracer
资金
- Basic Science Research Program through the National Research Foundation of Korea (NRF) - Ministry of Science, ICT and Future Planning [NRF-2014R1A2A2A0300740]
- Nuclear Research & Development Program through the National Research Foundation of Korea (NRF) - Ministry of Science, ICT and Future Planning [NRF-2013M2A2A7059471]
- Inha University [INHA-49297-01]
- National Research Foundation of Korea [2011-0030164] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
To expand the applications of positron emission tomography (PET), novel specific radiopharmaceuticals using positron-emitters, such as fluorine-18 (F-18, t(1/2) = 109.8 min), will be needed. Recently, strain-promoted alkyne azide cycloaddition (SPAAC) ha been considered as an alternative bioorthogonal conjugation reaction between bioactive molecules and radiolabeled building blocks for the synthesis of novel radiopharmaceuticals. This mini-review provides a rapid overview of the emerging synthetic strategies based on the copper-free SPAAC conjugation reaction under physiologically-friendly reaction conditions for the high-throughput synthesis of F-18-labeled peptide tracers. Furthermore, an efficient mesoporous silica nanoparticles (MSNs) pretargeting for PET imaging were also introduced through the in situ bioorthogonal SPAAC labeling reaction by forming F-18-labeled MSNs at the tumor site in a living specimen. (C) 2015 Elsevier B.V. All rights reserved.
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