Work

The Growing Impact of Bioorthogonal Click Chemistry on the Development of Radiopharmaceuticals

Year: 2013

Type: article

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.

Source: Journal of Nuclear Medicine

DOI: 10.2967/jnumed.112.115550

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

Institutions: University of Pittsburgh, Memorial Sloan Kettering Cancer Center

Language: English

Topic: Radiopharmaceutical Chemistry and Applications

Subfield: Radiology, Nuclear Medicine and Imaging

Field: Medicine

Domain: Health Sciences

Open Access status: bronze

Funder: National Cancer Institute

Awards: PET Imaging of Topoisomerase-II Expression in Breast Cancer, Biomarkers for predicting response to Hsp90 therapy