Development of In-Tether Carbon Chiral Center-Induced Helical Peptide
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.
| Autor: | Hu, Kuan |
|---|---|
| ISBN: | 9789813366152 |
| Sprache: | Englisch |
| Seitenzahl: | 102 |
| Produktart: | Kartoniert / Broschiert |
| Verlag: | Springer Singapore |
| Veröffentlicht: | 27.01.2022 |
| Untertitel: | Methodology and Applications |
| Schlagworte: | Cell permeability Chirality Helicity Protein-Ligand Interactions Protein-protein interactions Self-assembly Stabilized peptide Staple peptide biochemical engineering |