Cell penetrating peptides (CPP) are peptides of 10 to 30 residues derived from natural translocating proteins. Multivalency is known to enhance cellular uptake for the Tat peptide and closely related polycationic sequences. To test whether multivalency effects on cellular uptake might occur with other CPP types, we prepared multivalent versions of various CPP and evaluated their uptake in HeLa and CHO cells, intracellular localization, cytotoxicity and hemolysis.
Multivalency effects on uptake comparable to Tat were observed with TP10 (image) and Antp, which are attributable to their polycationic nature. The efficient synthetic protocol for these divalent CPP and their localization in the cytoplasm suggest that they might be useful for applications in cargo delivery into cells.

This work was carried out in the group of Prof. Jean-Louis Reymond.

References:

• G. A. Eggimann, S. Buschor, T. Darbre, J.-L. Reymond;
  "Convergent synthesis and cellular uptake of multivalent cell penetrating peptides derived from Tat, Antp, pVEC, TP10 and SAP"
  Org. Biomol. Chem., 11, 6717-6733, (2013); doi:10.1039/C3OB41023D.