1,2,3‐Triazoles as Amide Bond Mimics: Triazole Scan Yields Protease‐Resistant Peptidomimetics for Tumor Targeting

Abstract

The triazole makes the difference: Replacement of amide bonds in the backbone of peptides by 1,4-disubstituted 1,2,3-triazole isosteres affords peptidomimetics with retained receptor affinity and cell-internalization properties, enhanced proteolytic stability, and improved tumor-targeting capabilities.