title: The growing impact of bioorthogonal click chemistry on the development of radiopharmaceuticals.
abstract: 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 (18)F, (64)Cu, (111)In, and (99m)Tc.
authors.affiliation: Department of Radiology, Molecular Imaging Laboratory, University of Pittsburgh, Pittsburgh, Pennsylvania 15219, USA.
authors.forename: Dexing
authors.initials: D
authors.lastname: Zeng
authors.forename: Brian M
authors.initials: BM
authors.lastname: Zeglis
authors.forename: Jason S
authors.initials: JS
authors.lastname: Lewis
authors.forename: Carolyn J
authors.initials: CJ
authors.lastname: Anderson
mesh_terms: D000818:Animals; D057930:Click Chemistry / Q000379:methods*; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D011854:Radiochemistry; D019275:Radiopharmaceuticals / Q000737:chemistry*
chemical_list: D019275:Radiopharmaceuticals
keywords: click chemistry; radiochemistry