Change search
ReferencesLink to record
Permanent link

Direct link
Assessing the uptake kinetics and internalization mechanisms of cell-penetrating peptides using a quenched fluorescence assay
Stockholm University, Faculty of Science, Department of Neurochemistry. University of Tartu, Estonia.
Stockholm University, Faculty of Science, Department of Neurochemistry.
Stockholm University, Faculty of Science, Department of Neurochemistry. University of Tartu, Estonia.
Show others and affiliations
2010 (English)In: Biochimica et Biophysica Acta - Biomembranes, ISSN 0005-2736, E-ISSN 1879-2642, Vol. 1798, no 3, 338-343 p.Article in journal (Refereed) Published
Abstract [en]

Cell-penetrating peptides (CPPs) have shown great potency for cargo delivery both in vitro and in vivo. Different biologically relevant molecules need to be delivered into appropriate cellular compartments in order to be active, for instance certain drugs/molecules, e.g. antisense oligonucleotides, peptides, and cytotoxic agents require delivery into the cytoplasm. Assessing uptake mechanisms of CPPs can help to develop novel and more potent cellular delivery vectors, especially in cases when reaching a specific intracellular target requires involvement of a specific internalization pathway. Here we measure the overall uptake kinetics, with emphasis on cytoplasmic delivery, of three cell-penetrating peptides M918, TP10 and pVec using a quenched fluorescence assay. We show that both the uptake levels and kinetic constants depend on the endocytosis inhibitors used in the experiments. In addition, in some cases only the internalization rate is affected by the endocytosis inhibitors while the total uptake level is not and vice versa, which emphasizes importance of kinetic studies when assessing the uptake mechanisms of CPPs. Also, there seems to be a correlation between lower total cellular uptake and higher first-order rate constants. Furthermore, this may indicate simultaneous involvement of different endocytic pathways with different efficacies in the internalization process, as hypothesized but not shown earlier in an uptake kinetics assay.

Place, publisher, year, edition, pages
2010. Vol. 1798, no 3, 338-343 p.
Keyword [en]
Cell-penetrating peptide, Uptake kinetic, Uptake mechanism, Endocytosis inhibitor
National Category
Biochemistry and Molecular Biology
URN: urn:nbn:se:su:diva-39088DOI: 10.1016/j.bbamem.2009.11.001ISI: 000275843700005OAI: diva2:318340
Available from: 2010-05-07 Created: 2010-05-07 Last updated: 2015-04-21Bibliographically approved

Open Access in DiVA

No full text

Other links

Publisher's full text

Search in DiVA

By author/editor
Eiríksdóttir, EmelíaLangel, Ülo
By organisation
Department of Neurochemistry
In the same journal
Biochimica et Biophysica Acta - Biomembranes
Biochemistry and Molecular Biology

Search outside of DiVA

GoogleGoogle Scholar
The number of downloads is the sum of all downloads of full texts. It may include eg previous versions that are now no longer available

Altmetric score

Total: 20 hits
ReferencesLink to record
Permanent link

Direct link