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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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Fluoroalkylation promotes cytosolic peptide delivery
Guangyu Rong1, Changping Wang2, Lijie Chen1
1Shanghai Key Laboratory of Regulatory Biology, East China Normal University, Shanghai 200241, China.
Science Advances
|August 28, 2020
Summary
Researchers developed a novel fluorination strategy to improve peptide delivery into the cytosol. This method enhances peptide stability and therapeutic efficacy, showing promise for cancer treatment by inhibiting tumor growth.
Area of Science:
- Biochemistry and Molecular Biology
- Nanotechnology
- Drug Delivery Systems
Background:
- Cytosolic delivery of peptides is hindered by enzymatic degradation and intracellular barriers.
- Existing peptide delivery methods often lack efficiency and stability.
Purpose of the Study:
- To develop a novel strategy for efficient and stable cytosolic delivery of peptides.
- To evaluate the therapeutic potential of fluorous-tagged peptides in vitro and in vivo.
Main Methods:
- Decoration of cargo peptides with a fluorous tag.
- Assembly of fluorous-tagged peptides into nanostructures.
- Assessment of cellular uptake, endosomal escape, and cytosolic release.
- Evaluation of enzymatic stability and functional restoration of delivered peptides.
- In vivo tumor growth inhibition assay using a fluorous-tagged proapoptotic peptide.
Main Results:
- Fluorous-tagged peptides were efficiently internalized and released into the cytosol.
- Nanostructures demonstrated enhanced stability against enzymatic degradation.
- The strategy significantly improved delivery efficiency compared to non-fluorinated analogs.
- Fluorous-tagged proapoptotic peptide effectively inhibited tumor growth in vivo.
Conclusions:
- Fluorination strategy offers an efficient approach for peptide cytosolic delivery.
- This method overcomes enzymatic degradation and intracellular barriers.
- Fluorous-tagged peptides hold significant potential for cancer therapy and other applications.
