期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 57, 期 39, 页码 12733-12736出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201806966
关键词
F-18-fluorination; photocatalysis; peptides; PET imaging; radiolabeling
资金
- NSERC Discovery Grant
- MSFHR Career Investigator Award
- MSFHR I2I Grant
- Hoffmann-La Roche Fellowship
- CCSRI Innovation Grant
- National Research Council of Canada
Peptides are often ideal ligands for diagnostic molecular imaging due to their ease of synthesis and tuneable targeting properties. However, labelling unmodified peptides with F-18 for positron emission tomography (PET) imaging presents a number of challenges. Here we show the combination of photoactivated sodium decatungstate and [F-18]-N-fluorobenzenesulfonimide effects site-selective F-18-fluorination at the branched position in leucine residues in unprotected and unaltered peptides. This streamlined process provides a means to directly convert native peptides into PET imaging agents under mild aqueous conditions, enabling rapid discovery and development of peptide-based molecular imaging tools.
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