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Article

Improving Membrane Activity and Cargo Delivery Efficacy of a Cell-Penetrating Peptide by Loading with Carboranes

1
Institute for Biochemistry, Department of Chemistry, University of Cologne, Zülpicher Str. 47a, 50674 Cologne, Germany
2
Pharmaceutical Chemistry I & II, Pharmaceutical Institute, Faculty of Mathematics and Natural Sciences, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany
*
Author to whom correspondence should be addressed.
Academic Editors: Prisca Boisguérin and Sébastien Deshayes
Pharmaceutics 2021, 13(12), 2075; https://doi.org/10.3390/pharmaceutics13122075
Received: 27 October 2021 / Revised: 17 November 2021 / Accepted: 1 December 2021 / Published: 3 December 2021
Cell-penetrating peptides (CPPs) have emerged as versatile tools to increase the intracellular accumulation of different kinds of cargoes. For an efficient cellular uptake and drug delivery, their organization into a distinct and stable secondary structure at the outer surface of the plasma membrane is a hallmark and supports optimal lipid–peptide interactions. Incorporation of hydrophobic moieties, such as carboranes (CBs), has the potential to increase the lipophilicity of peptides, and thus, to facilitate the formation of secondary structures. Herein, we present synthesis and biophysical as well as biological characterization of carborane-CPP conjugates having incorporated one or more CB clusters. Our results highlight the possibility to modulate the secondary structure of CPPs by the addition of CB’s leading to constructs with altered membrane activity and promising use in terms of nucleic acid delivery. View Full-Text
Keywords: alpha-helix stabilization; secondary structure; cell-penetrating peptides; lipid–peptide interaction; peptide engineering alpha-helix stabilization; secondary structure; cell-penetrating peptides; lipid–peptide interaction; peptide engineering
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MDPI and ACS Style

Lützenburg, T.; Burdina, N.; Scholz, M.S.; Neundorf, I. Improving Membrane Activity and Cargo Delivery Efficacy of a Cell-Penetrating Peptide by Loading with Carboranes. Pharmaceutics 2021, 13, 2075. https://doi.org/10.3390/pharmaceutics13122075

AMA Style

Lützenburg T, Burdina N, Scholz MS, Neundorf I. Improving Membrane Activity and Cargo Delivery Efficacy of a Cell-Penetrating Peptide by Loading with Carboranes. Pharmaceutics. 2021; 13(12):2075. https://doi.org/10.3390/pharmaceutics13122075

Chicago/Turabian Style

Lützenburg, Tamara, Nele Burdina, Matthias S. Scholz, and Ines Neundorf. 2021. "Improving Membrane Activity and Cargo Delivery Efficacy of a Cell-Penetrating Peptide by Loading with Carboranes" Pharmaceutics 13, no. 12: 2075. https://doi.org/10.3390/pharmaceutics13122075

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