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. 

Mehr Informationen
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