Cyclic peptides with heterocycles are cell membrane-permeable

Peptides, including cyclic peptides, generally don’t cross cell membranes easily, a property that has limited their use in medicine. Researchers have now boosted the drug potential of cyclic peptides by incorporating a heterocycle into their rings. Andrei Yudin and coworkers at the University of Toronto adapted an existing reaction to convert linear peptides into the heterocycle-containing peptidomimetics (Nat. Chem. 2016, DOI: 10.1038/nchem.2636). The one-step reaction of a linear peptide . . .