Journal
JOURNAL OF NUCLEAR MEDICINE
Volume 54, Issue 6, Pages 829-832Publisher
SOC NUCLEAR MEDICINE INC
DOI: 10.2967/jnumed.112.115550
Keywords
click chemistry; radiochemistry
Funding
- NCI NIH HHS [F32 CA144138, R01 CA172546] Funding Source: Medline
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Click chemistry has become a ubiquitous chemical tool with applications in nearly all areas of modern chemistry, including drug discovery, bioconjugation, and nanoscience. Radiochemistry is no exception, as the canonical Cu(I)- catalyzed azide-alkyne cycloaddition, strain-promoted azide-alkyne cycloaddition, inverse electron demand Diels-Alder reaction, and other types of bioorthogonal click ligations have had a significant impact on the synthesis and development of radiopharmaceuticals. This review will focus on recent applications of click chemistry ligations in the preparation of imaging agents for SPECT and PET, including small molecules, peptides, and proteins labeled with radionuclides such as F-18, Cu-64, In-111, and Tc-99m.
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