Innovative Peptide Bioconjugation Chemistry with Radionuclides: Beyond Classical Click Chemistry

<b>Background</b>: The incorporation of radionuclides into peptides and larger biomolecules requires efficient and sometimes biorthogonal reaction conditions, to which click chemistry provides a convenient approach. <b>Methods</b>: Traditionally, click-based radiolabeling tec...

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Main Authors: Samantha Leier (Author), Frank Wuest (Author)
Format: Book
Published: MDPI AG, 2024-09-01T00:00:00Z.
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Summary:<b>Background</b>: The incorporation of radionuclides into peptides and larger biomolecules requires efficient and sometimes biorthogonal reaction conditions, to which click chemistry provides a convenient approach. <b>Methods</b>: Traditionally, click-based radiolabeling techniques have focused on classical click chemistry, such as copper(I)-catalyzed alkyne-azide [3+2] cycloaddition (CuAAC), strain-promoted azide-alkyne [3+2] cycloaddition (SPAAC), traceless Staudinger ligation, and inverse electron demand Diels-Alder (IEDDA). <b>Results</b>: However, newly emerging click-based radiolabeling techniques, including tyrosine-click, sulfo-click, sulfur(VI) fluoride exchange (SuFEx), thiol-ene click, azo coupling, hydrazone formations, oxime formations, and RIKEN click offer valuable alternatives to classical click chemistry. <b>Conclusions</b>: This review will discuss the applications of these techniques in peptide radiochemistry.
Item Description:10.3390/ph17101270
1424-8247