Uptake kinetics of cell-penetrating peptides.

Journal article

As our knowledge increases about the diversity in uptake mechanisms displayed by cell-penetrating peptides (CPP), the concept of CPP uptake kinetics becomes increasingly complex. Here, we present three different assays that can be used for studying different kinetic aspects of CPP-mediated delivery: intracellular accumulation and membranolytical effects, intracellular CPP-cargo detachment, and finally a functional readout of a biological action from the delivered cargo. Unlike the traditional end-point measurements that give a static postincubation readout, these assays are all dynamic, real-time, in situ measurements obtained during incubation. A combination of some (or all) of these different assays gives us not only interesting kinetic information about the uptake routes but also provides a simple and valuable methodology for the evaluation of potential drug candidates based on the chemical modification of CPPs by cargo attachment.

Authors: Florén, A; Mäger, I; Langel, U

• Journal: Methods in molecular biology (Clifton, N.J.)
• Volume: 683
• Pages: 117-128
• Publication date: 2011-01-01
• DOI: 10.1007/978-1-60761-919-2_9
• EISSN: 1940-6029
• ISSN: 1064-3745
• Language: English
• Keywords: Hela Cells; Cell-Penetrating Peptides; Spectrometry, Fluorescence; Kinetics; Temperature; Fluorescent Dyes; Protein Transport; Intracellular Space; Humans