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Updated: Jul 7, 2025
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Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
Published on: September 19, 2022
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Cell-Penetrating Peptide-Bismuth Bicycles.
Saan Voss1,2, Liam D Adair3,4, Katharina Achazi5
1Research School of Chemistry, Australian National University, Canberra, ACT 2601, Australia.
Angewandte Chemie (International Ed. in English)
|December 21, 2023
Summary
We developed novel peptide-bismuth bicycles as cell-penetrating peptides (CPPs) for enhanced cargo delivery into human cells. These bicyclic CPPs show significantly higher cellular uptake than traditional CPPs like TAT peptide or octaarginine.
Area of Science:
- Biochemistry
- Cell Biology
- Nanotechnology
Background:
- Cell-penetrating peptides (CPPs) are crucial for intracellular delivery.
- Existing CPPs like TAT peptide and octaarginine have limitations in efficiency and charge requirements.
Purpose of the Study:
- To develop and characterize novel CPPs based on peptide-bismuth bicycles.
- To evaluate the cellular uptake efficiency of these new CPPs compared to conventional ones.
Main Methods:
- Synthesis of peptide-bismuth bicycles from commercial peptide precursors.
- Live-cell confocal microscopy with fluorescently labeled peptides.
- Inductively coupled plasma mass spectrometry (ICP-MS) for quantifying intracellular bismuth.
Main Results:
- Demonstrated cellular entry of peptide-bismuth bicycles into human cells.
- Achieved significantly higher cellular uptake (over one order of magnitude) compared to TAT peptide and octaarginine.
- Confirmed intracellular presence of bismuth using ICP-MS, validating an alternative uptake analysis method.
Conclusions:
- Peptide-bismuth bicycles represent a new class of highly efficient CPPs.
- Bicyclization induced by bismuth(III) dramatically enhances cellular uptake.
- Cellular uptake mechanism is energy-dependent and likely involves macropinocytosis.
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