A Cross-Stitched Peptide with Improved Helicity and Proteolytic Stability

摘要

A new computational approach to obtain quantitative energy profiles for helix folding was used in the design of orthogonal hydrocarbon and lactam bicyclic peptides. The proteolytically stable,“cross-stitched” peptide SRC2-BCP1 shows nanomolar affinity for estrogen receptor α and x-ray crystallography confirms a helical binding pose.