Department of Radiology, Molecular Imaging Laboratory, University of Pittsburgh, Pittsburgh, Pennsylvania 15219, USA.
J Nucl Med. 2013 Jun;54(6):829-32. doi: 10.2967/jnumed.112.115550. Epub 2013 Apr 24.
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.
点击化学已成为一种无处不在的化学工具,几乎应用于现代化学的所有领域,包括药物发现、生物缀合和纳米科学。放射化学也不例外,因为经典的 Cu(I)催化的叠氮-炔环加成、应变促进的叠氮-炔环加成、逆电子需求 Diels-Alder 反应和其他类型的生物正交点击连接对放射性药物的合成和发展产生了重大影响。这篇综述将重点介绍点击化学连接在制备 SPECT 和 PET 成像剂方面的最新应用,包括用放射性核素(如 (18)F、(64)Cu、(111)In 和 (99m)Tc 标记的小分子、肽和蛋白质。