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Cell-Penetrating, Peptide-Based RAFT Agent for Constructing Penetration Enhancers
Chao Chen1, Friederike Richter2,3, Carlos Guerrero-Sanchez2,3
1Beijing Advanced Innovation Center for Soft Matter Science and Engineering; College of Materials Science and Engineering, Beijing University of Chemical Technology, Beijing 100029, China.
ACS Macro Letters
|May 31, 2022
Summary
Researchers created novel peptide-polymer conjugates using a cell-penetrating peptide (Transportan 10) and reversible addition-fragmentation chain transfer polymerization. These conjugates effectively penetrate cells, showing promise for drug and gene delivery applications.
Area of Science:
- Polymer Chemistry
- Bioconjugation
- Nanotechnology
Background:
- Peptide-polymer conjugates offer solutions for therapeutic and diagnostic limitations of peptides.
- Well-defined conjugates are crucial for developing functional drugs and gene delivery systems.
Purpose of the Study:
- To design and synthesize novel peptide-polymer conjugates using a sequence-defined cell-penetrating peptide.
- To create amphiphilic block copolymers with cell-penetrating capabilities for enhanced delivery.
Main Methods:
- Automated peptide synthesis of a Transportan 10 (TP 10)-based chain transfer agent (TP-CTA).
- Reversible addition-fragmentation chain transfer (RAFT) polymerization to synthesize poly[oligo(ethylene glycol) methyl ether acrylate]-block-poly(n-butyl acrylate) (TP-POEGA-b-PBA) using TP-CTA.
- Circular dichroism (CD) spectroscopy and transmission electron microscopy (TEM) for characterization.
Main Results:
- Confirmation of the preserved α-helix structure of TP 10 using CD spectroscopy, crucial for bioactivity.
- TEM revealed self-assembled nanostructures (rods and vesicles) in aqueous environments.
- Demonstrated effective cell penetration by the synthesized peptide-conjugated block copolymers.
Conclusions:
- A novel method for synthesizing peptide-polymer conjugates with cell-penetrating abilities was successfully developed.
- The synthesized TP-POEGA-b-PBA conjugates show significant potential for applications in drug and gene delivery.
- Preservation of peptide bioactivity within the polymer conjugate is achievable.
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