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Drug Design Reviews - Online (Discontinued)


ISSN (Print): 1567-2697
ISSN (Online): 1567-2697

Cellular Uptake of Cell-Penetrating Peptides

Author(s): E. Eiríksdottir, H. Myrberg, M. Hansen and U. Langel

Volume 1, Issue 2, 2004

Page: [161 - 173] Pages: 13

DOI: 10.2174/1567269043480636

Price: $65


Cellular machinery is protected from the surrounding by two-layer lipid membrane that is impermeable for most substances unnecessary for cellular metabolism. Unfortunately, from a cellular point of view, most new generation drugs, designed to act on gene regulation and transcription, are also considered to be unnecessary for metabolism and therefore showing poor, if any, intracellular localization. To overcome this obstacle, several chemical and physical methods have been developed, improving the uptake, but, on the other hand, also showing some unwanted side effects or limitations for in vivo applications. This dictates the continuing need for improved drug delivery and one way seems to be the relatively new class of compounds - cell-penetrating peptides (CPPs). Discovered approximately a decade ago, the content of this class is growing rapidly, containing now more than 100 compounds, which shows the intensity of work in this field. CPPs have already been shown to translocate cellular membranes in an unknown, seemingly receptor-independent and non-endocytotic manner. Moreover, they are able to deliver cargoes exceeding their own size up to 100-fold into a cellular milieu both in vitro and in vivo. The variety of different cargoes includes, but is not limited to: DNA, antisense PNA, oligonucleotides and small proteins. Recent data argues though that endocytosis is involved and contributes in some cases to the main part of the translocation. This review summarizes data on mechanisms of cell-penetrating peptides.

Keywords: cell-penetrating peptides, translocation, internalization, fixation, endocytosis

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