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

Journal of Nuclear Medicine

Brian M. Zeglis¹  Jason S. Lewis¹  Carolyn J. Anderson¹  Dexing Zeng¹ 

关键词: click chemistry;    radiochemistry;   

DOI  :  10.2967/jnumed.112.115550

学科分类：医学（综合）

来源: Society of Nuclear Medicine

【 摘 要 】

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.

【 授权许可】

Unknown