SialoPen peptides are new cationic foldamers with remarkable cell permeability

Heliyon

Erik M. Contreras¹  Hector C. Aguilar¹  Jonel P. Saludes²  Gary A. Wayman³  I. Abrrey Monreal³ 

[1] Department of Chemistry, Washington State University, Pullman, WA 99164, USA;Department of Integrative Physiology and Neuroscience, Washington State University, Pullman, WA 99164, USA;Immunology and Microbiology Department, Cornell University, Ithaca, NY 14850, USA;

关键词: Cell penetrating peptides;    Foldamer;    Sialic acid;    Polymer;    SPPS;    Drug delivery;   

DOI  :  

来源: DOAJ

【 摘 要 】

The ability to access intracellular targets is of vital importance as the number of identified druggable intracellular targets increases every year. However, intracellular delivery poses a formidable barrier, as many potential therapeutics are impermeable to cell membranes, which hinders their practical application in drug development. Herein we present de novo-designed unnatural cell penetrating peptide foldamers utilizing a 2,3-Didehydro-2-deoxyneuraminic acid (Neu2en) scaffold. Conveniently, this scaffold is amenable to standard Fmoc-based solid-phase peptide synthesis, with the advantages of tunable secondary structures and enhanced biostability. Flow cytometry and live-cell confocal microscopy studies showed that these Neu2en-based peptides, hereinafter termed SialoPen peptides, have significantly superior uptake in HeLa and primary neuronal hippocampal cells, outperforming the classical cell permeable peptides penetratin and HIV-TAT.

【 授权许可】

Unknown