Year: 2020
Type: article
Abstract: 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.
Source: Heliyon
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: gold
Estimated APC paid: $1,750
Funders: National Science Foundation, M.J. Murdock Charitable Trust, EMC, Washington State University, Department of Science and Technology, Philippines, National Institutes of Health, NIH Office of the Director, National Institute of General Medical Sciences, National Institute of Allergy and Infectious Diseases, National Center for Research Resources, Eunice Kennedy Shriver National Institute of Child Health and Human Development
Awards: Acquisition of a 300 MHz NMR Spectrometer, AQUISITION OF A 600 MHZ NMR SPECTROMETER, G2131920584, MRI: Acquisition of Instrumentation for Spatially Relevant Plant Metabolomics and Proteomics, A 500 MHz NMR Spectrometer Upgrade for Structural Biology, Mechanisms of Nipah virus fusion and entry, G4445522520, G491185128, G5617272702, Training in Biotechnology: Emphasis in Protein Chemistry, Leptin regulation of GABAergic synaptogenesis and excitation-inhibition balance during development: effects of maternal obesity, G859742517, G8679654653
OpenAlex ID: W3114079993