Journal
MOLECULAR PHARMACEUTICS
Volume 9, Issue 5, Pages 1529-1534Publisher
AMER CHEMICAL SOC
DOI: 10.1021/mp300070w
Keywords
gamma-AApeptides; cellular uptake; peptidomimetics; Tat; cell penetrating peptide (CPP)
Funding
- USF
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Cell-penetrating peptides including the trans-activating transcriptional activator (Tat) from HIV-1 have been used as carriers for intracellular delivery of a myriad of cargoes including drugs, molecular probes, DNAs and nanoparticles. Utilizing fluorescence flow cytometry and confocal fluorescence microscopy, we demonstrate that a gamma-AApeptide mimetic of Tat (48-57) can cross the cell membranes and enter the cytoplasm and nucleus of cells, with efficiency comparable to or better than that of Tat peptide (48-57). Deletion of the four side chains of the gamma-AApeptide attenuates translocation capability. We also establish that the gamma-AApeptide is even less toxic than the Tat peptide against mammalian cells. In addition to their low toxicity, gamma-AApeptides are resistant to protease degradation, which may prove to be advantageous over alpha-peptides for further development of molecular transporters for intracellular delivery.
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