Probing length effects and mechanism of cell penetrating agents mounted on a polyproline helix scaffold

Bioorg Med Chem Lett. 2007 May 15;17(10):2765-8. doi: 10.1016/j.bmcl.2007.02.077. Epub 2007 Mar 3.

Abstract

Cell penetrating peptides (CPP) displaying a type II polyproline helix backbone of different length and amphiphilic character were synthesized and their cellular uptake was compared. The longer CPP sequence, P14LRR, displayed a 7- to 12-fold higher uptake in MCF-7 cells as compared to its shorter counterpart, P11LRR, and a 35-fold higher uptake as compared to Tatp. These results demonstrate that an increased number of cationic and hydrophobic residues can strongly influence the extent of cellular internalization. Mechanistic investigations suggest internalization via a receptor independent endocytotic pathway with these agents.

MeSH terms

  • Endocytosis
  • Hydrophobic and Hydrophilic Interactions
  • Molecular Probe Techniques
  • Peptides / chemistry*
  • Peptides / pharmacology
  • Protein Structure, Secondary*
  • Tumor Cells, Cultured

Substances

  • Peptides
  • polyproline