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Updated: Dec 8, 2025

Antimicrobial Peptides Produced by Selective Pressure Incorporation of Non-canonical Amino Acids
Published on: May 4, 2018
Development of Peptides that Inhibit Aminoglycoside-Modifying Enzymes and β-Lactamases for Control of Resistant
Bruna O Costa1, Marlon H Cardoso1, Octávio L Franco1
1S-inova Biotech, Programa de Pós-Graduação em Biotecnologia, Universidade Católica Dom Bosco, Campo Grande - MS, 79117900, Brazil.
Abstract:
Aminoglycosides and β-lactams are the most commonly used antimicrobial agents in clinical practice. This occurs because they are capable of acting in the treatment of acute bacterial infections. However, the effectiveness of antibiotics has been constantly threatened due to bacterial pathogens producing resistance enzymes. Among them, the aminoglycoside-modifying enzymes (AMEs) and β-lactamase enzymes are the most frequently reported resistance mechanisms. AMEs can inactivate aminoglycosides by adding specific chemical molecules in the compound, whereas β-lactamases hydrolyze the β-lactams ring, preventing drug-target interaction. Thus, these enzymes provide a scenario of multidrug-resistance and a significant threat to public health at a global level. In response to this challenge, in recent decades, several studies have focused on the development of inhibitors that can restore aminoglycosides and β-lactams activity. In this context, peptides appear as a promising approach in the field of inhibitors for future antibacterial therapies, as multiresistant bacteria may be susceptible to these molecules. Therefore, this review focused on the most recent findings related to peptide-based inhibitors that act on AMEs and β-lactamases, and how these molecules could be used for future treatment strategies.
Insights
Peptides show promise as inhibitors against bacterial resistance enzymes like aminoglycoside-modifying enzymes (AMEs) and β-lactamases. These peptide-based inhibitors could restore the effectiveness of essential antibiotics, aminoglycosides and β-lactams, against multidrug-resistant bacteria.
Area of Science:
- Microbiology
- Biochemistry
- Drug Discovery
Background:
- Aminoglycosides and β-lactams are crucial antibiotics for treating bacterial infections.
- Bacterial resistance enzymes, specifically aminoglycoside-modifying enzymes (AMEs) and β-lactamases, significantly reduce antibiotic efficacy.
- This resistance poses a global public health threat, necessitating novel therapeutic strategies.
Purpose of the Study:
- To review recent advancements in peptide-based inhibitors targeting AMEs and β-lactamases.
- To explore the potential of these peptide inhibitors in combating multidrug-resistant bacteria.
- To discuss future applications of peptide inhibitors in antibacterial treatment strategies.
Main Methods:
- Literature review of recent scientific findings.
- Analysis of peptide structures and mechanisms of action against resistance enzymes.
- Evaluation of the potential of peptides to restore antibiotic activity.
Main Results:
- Peptides are emerging as effective inhibitors of AMEs and β-lactamases.
- These peptide inhibitors demonstrate the ability to counteract key bacterial resistance mechanisms.
- Multidrug-resistant bacteria show susceptibility to certain peptide-based therapeutic approaches.
Conclusions:
- Peptide-based inhibitors represent a promising strategy to overcome antibiotic resistance.
- Further research into peptide inhibitors could lead to new treatments for infections caused by resistant bacteria.
- Peptides offer a potential solution to restore the clinical utility of essential antibiotics like aminoglycosides and β-lactams.
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