Relationships between Membrane Binding, Affinity and Cell Internalization Efficacy of a Cell-Penetrating Peptide: Penetratin as a Case Study
2011

How Penetratin Interacts with Cell Membranes

Sample size: 1000000 publication 10 minutes Evidence: moderate

Author Information

Author(s): Isabel D. Alves, Cherine Bechara, Astrid Walrant, Yefim Zaltsman, Chen-Yu Jiao, Sandrine Sagan

Primary Institution: UPMC Univ Paris 06, UMR 7203, LBM, Paris, France

Hypothesis

Does the interaction of penetratin with cell surface components affect its internalization efficacy?

Conclusion

The study concludes that high-affinity binding of penetratin to cell membranes does not predict its internalization efficiency.

Supporting Evidence

  • Penetratin internalized with the same efficacy in three cell lines at 1 µM.
  • At 10 µM, penetratin was better internalized in SAneg cells compared to WT and GAGneg cells.
  • The affinity of penetratin for WT cells was 10 nM, while it was in the micromolar range for SAneg and GAGneg cells.

Takeaway

Penetratin is a special peptide that can enter cells, but just because it sticks to the outside of the cell doesn't mean it will get inside easily.

Methodology

The study used mass spectrometry to quantify internalized and membrane-bound penetratin in different cell lines and investigated binding affinity and kinetics using plasmon resonance and calorimetry.

Limitations

The sensitivity of the methods used limited the ability to measure very low concentrations of penetratin accurately.

Participant Demographics

The study involved three different cell lines: wild type (WT), glycosaminoglycans-deficient (GAGneg), and sialic acid-deficient (SAneg) CHO cells.

Statistical Information

P-Value

p<0.01

Statistical Significance

p<0.01

Digital Object Identifier (DOI)

10.1371/journal.pone.0024096

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