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Cationic cell-penetrating peptides induce ceramide formation via acid sphingomyelinase: implications for uptake.
TLDR
It is shown that a previously poorly understood mechanism of cationic CPP import depends on the ASMase-dependent formation of ceramide on the outer leaflet of the plasma membrane and this is the first illustration that a class of delivery vectors operates through the induction of an enzymatic activity that changes the lipid composition of the Plasma membrane. Expand
A Cell-penetrating Peptide Derived from Human Lactoferrin with Conformation-dependent Uptake Efficiency
TLDR
The identification and characterization of a 22-amino acid CPP derived from the human milk protein, lactoferrin is reported on, which exhibits a conformation-dependent uptake efficiency that is correlated with efficient binding to heparan sulfate and lipid-induced conformational changes. Expand
Multivalent design of apoptosis-inducing bid-BH3 peptide-oligosaccharides boosts the intracellular activity at identical overall peptide concentrations.
TLDR
Comparison of lowly multivalent and highly multivalent peptide dextrans proved a multivalency effect in life cells which was specific for the BH3 peptide sequence. Expand
Peptide microarrays to probe for competition for binding sites in a protein interaction network.
TLDR
Peptide microarrays enable the description of physiologically relevant binding patterns for proteins of interest and the identification of those peptide motifs, which are most strongly affected by competition. Expand
Simultaneous detection of intracellular target and off‐target binding of small molecule cancer drugs at nanomolar concentrations
TLDR
A combination of fluorescence correlation spectroscopy (FCS) and fluorescence cross‐correlation spectroscope (FCCS) is presented as a solution to the problem of off‐target binding and membrane permeability in vitro assays. Expand
The intracellular pharmacokinetics of terminally capped peptides.
TLDR
Analysis of the structure-activity relationship of peptides with respect to intracellular residence time and proteolytic breakdown provides a straightforward analytical access to a better understanding of the principles of peptide stability inside cells and will therefore greatly assist the development of bioactive peptides. Expand
HPMA as a scaffold for the modular assembly of functional peptide polymers by native chemical ligation.
TLDR
The cofunctionalization of a thioester-activated N-hydroxypropyl methacrylamide copolymer with the cell-penetrating peptide (CPP) nonaarginine and a bioactive peptide as independent building blocks by native chemical ligation is demonstrated. Expand
The in vitro biological activity of the HLA-DR-binding clinical IgG4 antibody 1D09C3 is a consequence of the disruption of cell aggregates and can be abrogated by Fab arm exchange.
TLDR
The results indicate that the activity of 1D09C3 in vitro may have been a consequence of assay design rather than an ability to induce HLA-DR-dependent cell death, and this antibody undergoes Fab arm exchange in the presence of IgG4. Expand
Measurements of the intracellular stability of CPPs.
TLDR
Fluorescence correlation spectroscopy (FCS) is introduced as a powerful method to address peptide stability in cells and cell lysates and provides direct information on peptide degradation and association with cellular structures in intact cells. Expand
Coupling to Polymeric Scaffolds Stabilizes Biofunctional Peptides for Intracellular Applications
TLDR
It is demonstrated that coupling to N-hydroxypropyl methacrylamide (HPMA) copolymer greatly enhances the activity of apoptosis-inducing peptides inside cells, revealing proteolytic protection as the basis for higher activity. Expand
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