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

The growing impact of bioorthogonal click chemistry on the development of radiopharmaceuticals.
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DOI:
10.2967/jnumed.112.115550
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发表时间:
2013-06
期刊:
Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子:
--
通讯作者:
Anderson CJ
Anderson CJ
中科院分区:
其他
文献类型:
--
作者:
Zeng D;Zeglis BM;Lewis JS;Anderson CJ

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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、生物共轭和纳米科学。放射化学也不例外,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、逆电子需求狄尔斯-阿尔德反应以及其他类型的生物正交点击连接对放射性药物的合成和开发产生了重大影响。本综述将重点关注点击化学连接在制备 SPECT 和 PET 显像剂中的最新应用,包括用 18F、64Cu、111In 和 99mTc 等放射性核素标记的小分子、肽和蛋白质。
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.
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