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Related Experiment Video

Updated: Feb 10, 2026

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
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Emerging Methods and Design Principles for Cell-Penetrant Peptides.

Leila Peraro1, Joshua A Kritzer1

  • 1Department of Chemistry, Tufts University, Medford, Massachusetts, 02155, USA.

Angewandte Chemie (International Ed. in English)
|May 10, 2018
PubMed
Summary
This summary is machine-generated.

This review explores chemical strategies for creating cell-penetrant peptides, essential for targeting intracellular proteins. It details methods like masking, patterning, and quantification for improved drug development.

Keywords:
cell-penetrating peptidescellular deliverycyclic peptidespeptide therapeutics

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Area of Science:

  • Chemical Biology
  • Drug Development
  • Molecular Biology

Background:

  • Biomolecules like peptides are crucial for chemical biology and drug discovery.
  • Targeting extracellular proteins is established, but intracellular protein access remains a challenge.

Purpose of the Study:

  • To review chemical strategies for developing cell-penetrant peptides.
  • To identify and analyze key approaches for enhancing peptide cell penetration.

Main Methods:

  • Discusses three distinct strategies: masking backbone amides, guanidinium group patterning, and amphipathic patterning.
  • Summarizes data sets providing design guidelines for each strategy.
  • Evaluates methods for quantifying peptide cell penetration.

Main Results:

  • Identified three primary strategies for creating cell-penetrant peptides.
  • Emerging data sets offer specific design principles for these strategies.
  • Current methods for quantifying cell penetration have varying advantages and disadvantages.

Conclusions:

  • Optimized cytosolic penetration of bioactive peptides is achievable through specific chemical design principles.
  • This review provides a framework for applying these methods to enhance intracellular drug delivery.