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Macrocyclic peptides

Tying up loose ends

Despite their potential as drugs, peptides are generally not cell permeable, which limits their practical applications in medicine. Now, linear peptides have been cyclized by using a heteroaromatic linker. This cyclization both improves passive membrane permeability and stabilizes a biologically relevant secondary structure.

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Figure 1: Synthesis of oxadiazole-containing cyclic peptides.

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Correspondence to Jeffrey W. Bode.

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Saito, F., Bode, J. Tying up loose ends. Nature Chem 8, 1085–1086 (2016). https://doi.org/10.1038/nchem.2683

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