Internalization mechanisms of cell-penetrating peptides

In today’s modern era of medicine, macromolecular compounds such as proteins, peptides and nucleic acids are dethroning small molecules as leading therapeutics. Given their immense potential, they are highly sought after. However, their application is limited mostly due to their poor in vivo stabili...

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Vydané v:Beilstein journal of nanotechnology Ročník 11; číslo 1; s. 101 - 123
Hlavní autori: Ruseska, Ivana, Zimmer, Andreas
Médium: Journal Article
Jazyk:English
Vydavateľské údaje: Germany Beilstein-Institut zur Föerderung der Chemischen Wissenschaften 2020
Beilstein-Institut
Predmet:
Amino acids
cell-penetrating peptides
Classification
direct translocation
drug delivery
endocytosis
HIV
Human immunodeficiency virus
internalization
Macromolecules
Membranes
Nanoscience
Nanotechnology
Nucleic acids
Peptides
Proteins
Review
Vectors (Biology)
endocytosis
internalization
drug delivery
cell-penetrating peptides
direct translocation
ISSN:2190-4286, 2190-4286
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Shrnutí:In today’s modern era of medicine, macromolecular compounds such as proteins, peptides and nucleic acids are dethroning small molecules as leading therapeutics. Given their immense potential, they are highly sought after. However, their application is limited mostly due to their poor in vivo stability, limited cellular uptake and insufficient target specificity. Cell-penetrating peptides (CPPs) represent a major breakthrough for the transport of macromolecules. They have been shown to successfully deliver proteins, peptides, siRNAs and pDNA in different cell types. In general, CPPs are basic peptides with a positive charge at physiological pH. They are able to translocate membranes and gain entry to the cell interior. Nevertheless, the mechanism they use to enter cells still remains an unsolved piece of the puzzle. Endocytosis and direct penetration have been suggested as the two major mechanisms used for internalization, however, it is not all black and white in the nanoworld. Studies have shown that several CPPs are able to induce and shift between different uptake mechanisms depending on their concentration, cargo or the cell line used. This review will focus on the major internalization pathways CPPs exploit, their characteristics and regulation, as well as some of the factors that influence the cellular uptake mechanism.
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ISSN:2190-4286
2190-4286
DOI:10.3762/bjnano.11.10