Cyclobutane-bearing restricted anchoring residues enabled geometry-specific hydrocarbon peptide stapling
Baobao Chen, Chao Liu, Wei Cong, Fei Gao, Yan Zou, Li Su, Lei Liu, Alexander Hillisch, Lutz Lehmann, Donald Bierer, Xiang Li, Honggang Hu
Abstract
geometry-specific stapled peptides indeed exhibit higher α-helicity and thus stronger biological activity than canonical hydrocarbon stapled peptides. We believe that this methodology possesses great potential to expand the scope of the existing peptide stapling strategy. These cyclobutane-bearing restricted anchoring residues served as effective supplements for the existing olefin-terminated unnatural amino acids and the resultant geometry-specific hydrocarbon peptide stapling provided more potential for peptide therapeutics.
Topics & Concepts
CyclobutaneChemistryPeptideAmino acidStereochemistryRational designCyclobutanesCombinatorial chemistryRing (chemistry)BiochemistryOrganic chemistryNanotechnologyMaterials scienceChemical Synthesis and AnalysisClick Chemistry and ApplicationsAntimicrobial Peptides and Activities