AI Article Synopsis
- Cell-penetrating peptides (CPPs) are short peptides that can transport various substances into cells but face challenges with vesicular entrapment during internalization.
- Modifying peptides, specifically longer oligoarginines, enhances their ability to directly enter the cytosol, with the study focusing on tetra- and hexaarginine modified with a Dabcyl group.
- The modified hexaarginine demonstrates improved cellular uptake and a diffuse distribution inside cells at lower concentrations, showing potential for use in antitumor drug delivery.
Article Abstract
Cell-penetrating peptides (CPPs) are promising delivery vehicles. These short peptides can transport wide range of cargos into cells, although their usage has often limitations. One of them is the endosomatic internalisation and thus the vesicular entrapment. Modifications which increases the direct delivery into the cytosol is highly researched area. Among the oligoarginines the longer ones (n > 6) show efficient internalisation and they are well-known members of CPPs. Herein, we describe the modification of tetra- and hexaarginine with (4-((4-(dimethylamino)phenyl)azo)benzoyl) (Dabcyl) group. This chromophore, which is often used in FRET system increased the internalisation of both peptides, and its effect was more outstanding in case of hexaarginine. The modified hexaarginine may enter into cells more effectively than octaarginine, and showed diffuse distribution besides vesicular transport already at low concentration. The attachment of Dabcyl group not only increases the cellular uptake of the cell-penetrating peptides but it may affect the mechanism of their internalisation. Their conjugates with antitumor drugs were studied on different cells and showed antitumor activity.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8241751 | PMC |
| http://dx.doi.org/10.1007/s00726-021-03003-w | DOI Listing |
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Article Synopsis
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- * Results indicate that these modified CPPs can deliver antitumor drugs effectively to cancer cell lines, with a notable ability to outperform established CPPs like octaarginine in terms of cell penetration.
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