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Updated: Jul 15, 2025

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
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Peptide Stapling Applied to Antimicrobial Peptides.

Ana Laura Pereira Lourenço1, Thuanny Borba Rios1,2, Állan Pires da Silva1

  • 1Programa de Pós-Graduação em Ciências Genômicas e Biotecnologia, Universidade Católica de Brasília, Brasília 71966-700, Brazil.

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|September 28, 2023
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Summary
This summary is machine-generated.

Stapled antimicrobial peptides (AMPs) show promise against drug-resistant microbes but face challenges. This review explores recent advances in stapled AMPs, focusing on overcoming limitations for therapeutic use.

Keywords:
all-hydrocarbon staplingantimicrobial peptidescyclizationstapling

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Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Microbiology

Background:

  • Antimicrobial peptides (AMPs) are vital in combating multi-drug resistant (MDR) microorganisms.
  • Proteolytic susceptibility limits AMP therapeutic applications.
  • Structural modifications, like cyclization, can enhance AMP stability and efficacy.

Purpose of the Study:

  • To review recent advancements in stapled antimicrobial peptides (AMPs) for antimicrobial applications.
  • To explore the potential of stapled AMPs as a future therapeutic strategy.
  • To understand the challenges and future directions for stapled AMPs.

Main Methods:

  • Review of recent scientific literature on stapled AMPs.
  • Analysis of various helix-stabilization techniques, including all-hydrocarbon stapling.
  • Evaluation of studies focusing on antimicrobial efficacy and stability.

Main Results:

  • All-hydrocarbon stapling is an effective strategy for constraining peptide helices, enhancing stability.
  • Despite stability benefits, toxicity remains a significant limitation for stapled AMPs.
  • Recent research shows progress in developing potent and stable stapled AMPs.

Conclusions:

  • Stapled AMPs offer a promising avenue for developing new antimicrobial agents against MDR pathogens.
  • Overcoming toxicity and optimizing stability are key for clinical translation of stapled AMPs.
  • Continued research into novel stapling strategies is crucial for realizing the therapeutic potential of AMPs.