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Keywords:

  • delivery systems;
  • peptides;
  • prodrugs;
  • rotaxanes;
  • supramolecular chemistry
Thumbnail image of graphical abstract

Ring of protection: A [2]rotaxane 1 protects and selectively releases a bioactive pentapeptide. The rotaxane macrocycle provides a defensive shield that very significantly improves the poor stability of the peptide to both individual peptidases and the cocktail of enzymes present in human plasma. Glycosidase-catalyzed cleavage of a carbohydrate ‘stopper’ in the rotaxane triggers release of the parent peptide (see picture).