The growing impact of bioorthogonal click chemistry on the development of radiopharmaceuticals

Dexing Zeng, Brian M. Zeglis, Jason S. Lewis, Carolyn J. Anderson

Research output: Contribution to journalReview articlepeer-review

87 Scopus citations


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 18F, 64Cu, 111In, and 99mTc.

Original languageEnglish (US)
Pages (from-to)829-832
Number of pages4
JournalJournal of Nuclear Medicine
Issue number6
StatePublished - Jun 1 2013
Externally publishedYes


  • Click chemistry
  • Radiochemistry

ASJC Scopus subject areas

  • Medicine(all)


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