Radio- And Fluorescent-Labeling Of Rituximab Based On The Inverse Electron Demand Diels-Alder Reaction

CHEMISTRYSELECT(2021)

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摘要
The bioorthogonal reaction between([1,2,4,5])tetrazines with trans-cyclooctene through the inverse electron demand Diels-Alder (IEDDA) has been described as powerful bioconjugation tool. In this work, we explore the IEDDA as a modular conjugation strategy for in vitro and in vivo labeling of Rituximab for the generation of radioactive and fluorescently label immunoconjugates. The strategy allowed the generation, in vitro and in vivo, of conjugated Rituximab with cyanine 5 and 7 and the gamma emmiter technetium-99m.
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关键词
Click chemistry, Fluorescent probes, Imaging agents, Radiopharmaceuticals, technetium
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