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Cargo delivery kinetics of cell-penetrating peptides

Academic Article
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Overview

authors

  • Hallbrink, M.
  • Floren, A.
  • Elmquist, A.
  • Pooga, M.
  • Bartfai, Tamas
  • Langel, Ülo

publication date

  • 2001

journal

  • Biochimica et Biophysica Acta-Biomembranes  Journal

abstract

  • A diversity of cell-penetrating peptides (CPPs), is known, but so far the only common denominator for these peptides is the ability to gain cell entry in an energy-independent manner. The mechanism used by CPPs for cell entry is largely unknown, and data comparing the different peptides are lacking. In order to gain more information about the cell-penetrating process, as well as to quantitatively compare the uptake efficiency of different CPPs, we have studied the cellular uptake and cargo delivery kinetics of penetratin, transportan, Tat (48-60) and MAP (KLAL). The respective CPPs (labelled with the fluorescence quencher, 3-nitrotyrosine) are coupled to small a pentapeptide cargo (labelled with the 2-amino benzoic acid fluorophore) via a disulfide bond. The cellular uptake of the cargo is registered as an increase in fluorescence intensity when the disulfide bond of the CPP-S-S-cargo construct is reduced in the intracellular milieu. Our data show that MAP has the fastest uptake, followed by transportan, Tat(48-60) and, last, penetratin. Similarly, MAP has the highest cargo delivery efficiency, followed by transportan, Tat (48-60) and, last, penetratin. Since some CPPs have been found to be toxic at high concentration, we characterized the influence of CPPs on cellular 2-[(3)H]deoxyglucose-6-phosphate leakage. Measurements on this system show that the membrane-disturbing potential appears to be correlated with the hydrophobic moment of the peptides. In summary, the yield and kinetics of cellular cargo delivery for four different CPPs has been quantitatively characterized.

subject areas

  • Amino Acid Sequence
  • Carrier Proteins
  • Cell Membrane Permeability
  • Cystine
  • Drug Carriers
  • Fluorescence
  • Galanin
  • Humans
  • Kinetics
  • Molecular Sequence Data
  • Oxidation-Reduction
  • Peptides
  • Recombinant Fusion Proteins
  • Tumor Cells, Cultured
  • Tyrosine
  • Wasp Venoms
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Research

keywords

  • cargo delivery kinetics
  • cell-penetrating peptides
  • cellular uptake
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Identity

International Standard Serial Number (ISSN)

  • 0005-2736

Digital Object Identifier (DOI)

  • 10.1016/s0005-2736(01)00398-4

PubMed ID

  • 11718666
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Additional Document Info

start page

  • 101

end page

  • 109

volume

  • 1515

issue

  • 2

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