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Updated: Jul 13, 2026
Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
Published on: September 19, 2022
A host-rotaxane derivatized with carboxylic acids efficiently delivers a highly cationic fluoresceinated peptide
Jing Zhu1, Brian E House, Erin Fleck
1Department of Chemistry, University of Cincinnati, Cincinnati, PO Box 210172, OH 45221, USA.
Abstract:
A cleft-[2]rotaxane (CR2+2-) was derivatized with carboxylic acids to enhance the intracellular delivery of a highly cationic or anionic pentapeptide. CR2+2- delivers the fluorescein (Fl) tagged peptide Fl-KKALR to a greater amount than Fl-QEAVD, and at a higher concentration, a greater amount than Fl-AVWAL. The level of delivery is largely temperature and ATP independent, suggesting that the Fl-peptide.CR2+2- complexes pass through the cellular membrane without requiring active cell-mediated processes. This study shows that selective delivery of peptides is possible by using a suitably derivatized host-rotaxane as the transporter.
