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

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181,89 

Methodology and Applications, Springer Theses

ISBN: 9813366125
ISBN 13: 9789813366121
Autor: Hu, Kuan
Verlag: Springer Verlag GmbH
Umfang: xv, 102 S., 10 s/w Illustr., 65 farbige Illustr., 102 p. 75 illus., 65 illus. in color.
Erscheinungsdatum: 27.01.2021
Auflage: 1/2021
Produktform: Gebunden/Hardback
Einband: Gebunden

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.

Artikelnummer: 378191 Kategorie:

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