Development of In-Tether Carbon Chiral Center-Induced Helical Peptide

Methodology and Applications
von Kuan Hu
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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. 

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ReiheSpringer Theses
ISBN 9789813366152
Sprache Englisch
Ausgabe 1st ed. 2021
Erscheinungsdatum 27.01.2022
Umfang 102 Seiten
Genre Chemie/Organische Chemie
Format Taschenbuch
Verlag Springer Singapore