1.

Record Nr.

UNINA9910484381203321

Autore

Hu Kuan

Titolo

Development of in-tether carbon chiral center-induced helical peptide : methodology and applications / / Kuan Hu

Pubbl/distr/stampa

Singapore : , : Springer, , [2021]

©2021

ISBN

981-336-613-3

Edizione

[1st ed. 2021.]

Descrizione fisica

1 online resource (XV, 102 p. 75 illus., 65 illus. in color.)

Collana

Springer Theses

Disciplina

547.756

Soggetti

Peptides - Synthesis

Cancer - Research

Peptides - Biotechnology

Chemistry Techniques, Synthetic

Peptides - therapeutic use

Peptides, Cyclic

Biomedical Research

Lingua di pubblicazione

Inglese

Formato

Materiale a stampa

Livello bibliografico

Monografia

Nota di contenuto

Introduction -- Method to construct in-tether chiral center constrained helical peptide -- Application in disrupting p53/MDM2 protein-protein interactions -- Fabrication of nanomaterials with in-tether chiral center constrained helical peptide.

Sommario/riassunto

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. .