Development of In-Tether Carbon Chiral Center-Induced Helical Peptide
Methodology and Applications
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Beschreibung
This book focuses on the development of stapled peptides, a novel molecular modality used to regulate aberrant intracellular protein–protein interactions (PPIs). The author designs and presents a novel helical peptide stabilization methodology by constructing a chiral cross-linker moiety, namely “chiral center induced peptide helicity (CIH)”. The book demonstrates that a precisely positioned carbon chiral center on tether can decisively determine the secondary structure of a peptide, and that the R-configured peptide is helical, while the S-configured peptide is non-helical. Further, it reports that helicity-enhanced R isomer peptides displayed significantly enhanced cell permeability and target binding affinity, as well as tumor inhibition efficiency, in comparison to S isomer peptides. The book will not only advance readers’ understanding of the basic principle of stapled peptides, but also accelerate the clinical transformation of stapled peptide drugs.
This book focuses on the development of stapled peptides, a novel molecular modality used to regulate aberrant intracellular protein–protein interactions (PPIs). The author designs and presents a novel helical peptide stabilization methodology by constructing a chiral cross-linker moiety, namely “chiral center induced peptide helicity (CIH)”. The book demonstrates that a precisely positioned carbon chiral center on tether can decisively determine the secondary structure of a peptide, and that the R-configured peptide is helical, while the S-configured peptide is non-helical. Further, it reports that helicity-enhanced R isomer peptides displayed significantly enhanced cell permeability and target binding affinity, as well as tumor inhibition efficiency, in comparison to S isomer peptides. The book will not only advance readers’ understanding of the basic principle of stapled peptides, but also accelerate the clinical transformation of stapled peptide drugs.
Nominated as an outstanding PhD thesis by Peking University Reports on important progress in the study of stabilized peptide drugs Introduces applications in cancer stem cell therapy and self-assembly for novel nanomaterials Includes a diversity-oriented synthesis methodology for constructing stabilized peptides and a clear study of the correlation between peptides’ structure and their biophysical/biochemical properties
Autor*in
Kuan Hu
Themen in »Development of In-Tether Carbon Chiral Center-Induced Helical Peptide«
Stabilized peptide Staple peptide Chirality Cell permeability Helicity Protein-protein interactions Self-assembly Protein-Ligand Interactions biochemical engineering