Proline-rich, amphipathic cell-penetrating peptides.
Proline-rich peptides are a chemically and structurally diverse family of cell-penetrating vectors characterised by the presence of pyrrolidine rings from prolines. Amphipathic Pro-rich peptides are particularly effective, demonstrating efficient cellular uptake and non-cytotoxicity. Derivatives with hydrophobic moieties, such as fatty acids or silaproline, have shown highly improved internalisation efficiency; an all D-amino acid version of the CPP SAP was shown to be completely protease resistant and was evaluated in a preliminary in vivo study. CD and TEM studies regarding the self-assembly properties of this family of peptides highlight the possible role of aggregated species in the internalisation process. Finally, these CPPs were shown to be internalised via caveolae or lipid-rafts mediated endocytosis, which circumvents the lysosomal route of degradation.
Pujals
Sílvia
S
Institute for Research in Biomedicine, Barcelona Science Park, University of Barcelona, Spain.
Giralt
Ernest
E
D000818:Animals; D002462:Cell Membrane / Q000378:metabolism; D002463:Cell Membrane Permeability; D002942:Circular Dichroism; D016503:Drug Delivery Systems / Q000379:methods; D006801:Humans; D046529:Microscopy, Electron, Transmission; D010455:Peptides / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D011392:Proline / Q000737:chemistry*; D011487:Protein Conformation; D021381:Protein Transport
D010455:Peptides; D011392:Proline