Consecutive click assembly enables rapid synthesis of PROTACs from ligands, suggesting a versatile bioactivity evaluation approach.
An efficient strategy to access proteolysis-targeting chimeras (PROTACs) is disclosed. Consecutive click assembly of readily available functional modules enables the rapid and modular synthesis of PROTACs. In this manuscript, we demonstrate the synthesis of a range of PROTACs from an E3 ligase ligand and an EGFR ligand, conveniently diversified with functional modules by triple-click assembly, together with evaluation of their bioactivity.
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Orimoto et al. (2025) studied this question.
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