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Link to original content: https://pubmed.ncbi.nlm.nih.gov/31398014
Stereoselective pH Responsive Peptide Dendrimers for siRNA Transfection - PubMed Skip to main page content
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. 2019 Aug 21;30(8):2165-2182.
doi: 10.1021/acs.bioconjchem.9b00403. Epub 2019 Aug 9.

Stereoselective pH Responsive Peptide Dendrimers for siRNA Transfection

Marc Heitz  1 , Sacha Javor  1 , Tamis Darbre  1 , Jean-Louis Reymond  1
Affiliations

Stereoselective pH Responsive Peptide Dendrimers for siRNA Transfection

Marc Heitz et al. Bioconjug Chem. .

Abstract

Transfecting nucleic acids into cells is an essential procedure in biological research usually performed using nonviral transfection reagents. Unfortunately, most transfection reagents have polymeric or undisclosed structures and require nonstandard synthetic procedures. Herein we report peptide dendrimers accessible as pure products from standard building blocks by solid-phase peptide synthesis and acting as nontoxic single component siRNA transfection reagents for a variety of cell lines with equal or better performance than the gold standard lipofectamine L2000. Structure-activity relationships and mechanistic studies illuminate their transfection mechanism in unprecedented detail. Stereoselective dendrimer aggregation via intermolecular β-sheets at neutral pH enables siRNA complexation to form nanoparticles which enter cells by endocytosis. Endosome acidification triggers protonation of amino termini and rearrangement to an α-helical conformation forming smaller dendrimer/siRNA nanoparticles, which escape the endosome and release their siRNA cargo in the cytosol. Two particularly efficient d-enantiomeric dendrimers are proposed as new reference reagents for siRNA transfection.

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