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Here we report a novel class of peptides-d-diaminopropionic acids (Dap)-for gene delivery. These peptides have attractive properties for gene delivery, and the advantage that they can be easily manipulated in relation to their composition, abiding with tailored-design. We characterized the toxicological and biophysical properties of DNA particles resulting from the interaction of the nucleic acid with a series of Dap(8) peptides conjugated to different alkyl groups. These peptides formed small and homogenous DNA particle populations that protected against DNase I degradation at non-toxic concentrations. However, despite the similarity between these peptides and others that are arginine-rich, and efficient vectors, functional studies suggest the need for additional modifications in the carriers to improve their DNA delivery efficiency. Taken together, these studies underscore the relevance of the overall structure of the carrier and the complexity of designing from scratch a carrier.

Original publication

DOI

10.1016/j.bmcl.2012.06.103

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/09/2012

Volume

22

Pages

5635 - 5638

Keywords

Animals, Cell Line, Cell Line, Tumor, Cell Survival, Cricetinae, DNA, Drug Carriers, Humans, Lipopeptides, Male, Mice, Mice, Inbred BALB C, Plasmids, Transfection, beta-Alanine