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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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Cyclic Cell-Penetrating Peptides with Single Hydrophobic Groups
Jian Song1,2, Ziqing Qian1, Ashweta Sahni1
1Department of Chemistry and Biochemistry, The Ohio State University, 484 West 12th Avenue, Columbus, Ohio, 43210, USA.
Chembiochem : a European Journal of Chemical Biology
|July 13, 2019
Summary
Researchers discovered new cyclic cell-penetrating peptides (CPPs) with a single hydrophobic residue. The lead peptide, CPP 17, shows superior cell entry in serum, offering a promising tool for drug delivery.
Area of Science:
- Biochemistry and Molecular Biology
- Peptide Chemistry
- Cellular Biology
Background:
- Cyclic cell-penetrating peptides (CPPs) are crucial for intracellular delivery.
- Existing cyclic CPPs often contain multiple hydrophobic residues, potentially limiting their efficacy.
- High serum protein concentrations can impede CPP activity due to protein binding.
Purpose of the Study:
- To discover and characterize a novel family of cyclic CPPs.
- To identify an optimal CPP structure for enhanced cellular uptake.
- To evaluate the performance of a lead CPP candidate under physiological conditions.
Main Methods:
- Synthesis and structural analysis of novel cyclic peptides.
- Assessment of cellular entry efficiency in vitro.
- Comparative analysis of CPP activity in the presence of varying serum protein concentrations.
Main Results:
- A new family of cyclic CPPs was identified, characterized by a single hydrophobic residue.
- The optimal structure comprises four arginine residues and a long-chain hydrophobic residue within a cyclohexapeptide ring.
- CPP 17, the most active peptide, exhibits comparable intrinsic cell entry to CPP12 but is 2.8 times more active in high serum, attributed to reduced protein binding.
- CPP 17 efficiently enters cells via direct translocation at concentrations as low as 5 μm.
Conclusions:
- A novel class of cyclic CPPs with a unique single hydrophobic residue motif has been developed.
- CPP 17 demonstrates superior performance in serum-rich environments compared to existing CPPs.
- This peptide represents a promising candidate for efficient and targeted intracellular delivery applications.
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