Journal
CHEMISTRY & BIOLOGY
Volume 18, Issue 8, Pages 1000-1010Publisher
CELL PRESS
DOI: 10.1016/j.chembiol.2011.06.006
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Funding
- Volkswagen Foundation (Nachwuchsgruppen an Universitaten) [1/77 472]
- Radboud University Nijmegen Medical Centre
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The use of protease-resistant D-peptides is a prominent strategy for overcoming proteolytic sensitivity in the use of cell-penetrating peptides (CPPs) as delivery vectors. So far, no major differences have been reported for the uptake of L- and D-peptides. Here we report that cationic L-CPPs are taken up more efficiently than their D-counterparts in MC57 fibrosarcoma and He La cells but not in Jurkat T leukemia cells. Reduced uptake of D-peptides co-occurred with persistent binding to heparan sulfates (HS) at the plasma membrane. In vitro binding studies of Land D-peptides with HS indicated similar binding affinities. Our results identify two key events in the uptake of CPPs: binding to HS chains and the initiation of internalization. Only the second event depends on the chirality of the CPP. This knowledge may be exploited for a stereochemistry-dependent preferential targeting of cells.
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