Fatty acyl moieties: improving Pro-rich peptide uptake inside HeLa cells.
In the field of drug delivery there has been a continuous study of powerful delivery systems to aid non permeable drugs in reaching their intracellular target. Among the systems explored are cell penetrating peptides (CPPs), which first garnered interest a decade ago when the interesting translocation properties of the pioneer CPPs Tat and Antp were described. A new family of CPPs has recently been described as non cytotoxic Pro-rich vectors with favorable profiles for internalization in HeLa cells. Fatty acyl moieties that can tune a peptide's interaction with the lipophilic environment of a cell membrane have been incorporated into the Pro-rich sequence. Improvements in cellular uptake of peptides modified with fatty acyl groups, as studied by confocal microscopy and flow cytometry, as well as the results obtained by the interaction of these peptides with a model dioleoylphosphatidylcholine (DOPC) membrane and transmission electron microscopy (TEM), illustrate the importance of the fatty acyl moieties for efficient internalization.
Fernández-Carneado
J
J
Institut de Recerca Biomèdica de Barcelona, Parc Científic de Barcelona, Josep Samitier 1, E-08028 Barcelona, Spain.
Kogan
M J
MJ
Van Mau
N
N
Pujals
S
S
López-Iglesias
C
C
Heitz
F
F
Giralt
E
E
D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics; D005227:Fatty Acids / Q000737:chemistry / Q000378:metabolism*; D005434:Flow Cytometry; D006367:HeLa Cells; D006801:Humans; D018613:Microscopy, Confocal; D046529:Microscopy, Electron, Transmission; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism*; D010713:Phosphatidylcholines; D011392:Proline / Q000737:chemistry / Q000378:metabolism*; D055232:Proline-Rich Protein Domains
D004337:Drug Carriers; D005227:Fatty Acids; D010455:Peptides; D010713:Phosphatidylcholines; D011392:Proline; C017251:1,2-oleoylphosphatidylcholine