Affiliation:
1. Department of Bioorganic Chemistry Leibniz Institute of Plant Biochemistry Weinberg 3 06120 Halle/Saale Germany
2. Laboratory of Synthetic and Biomolecular Chemistry Faculty of Chemistry University of Havana Zapata & G Havana 10400 Cuba
Abstract
AbstractMacrocyclization of peptides is typically used to fix specific bioactive conformations and improve their pharmacological properties. Recently, macrobicyclic peptides have received special attention owing to their capacity to mimic protein structures or be key components of peptide‐drug conjugates. Here, we describe the development of novel synthetic strategies for two distinctive types of peptide macrobicycles. A multicomponent macrocyclo‐dimerization approach is introduced for the production of interconnected β‐turns, allowing two macrocyclic rings to be formed and dimerized in one pot. Also, an on‐resin double stapling strategy is described for the assembly of lactam‐bridged macrobicycles with stable tertiary folds.
Subject
Organic Chemistry,Molecular Biology,Molecular Medicine,Biochemistry