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Updated: Jan 11, 2026
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Sequence-specific and Selective Recognition of Double-stranded RNAs over Single-stranded RNAs by Chemically Modified Peptide Nucleic Acids
Published on: September 21, 2017
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Aminoglycoside-Peptide Nucleic Acid (PNA) Conjugates against Gram-Negative Bacteria
Izabela Siekierska1, Joanna Trylska1
1University of Warsaw, Centre of New Technologies, 02-097 Warsaw, Poland.
Bioconjugate Chemistry
|November 19, 2025
Summary
Novel aminoglycoside-peptide nucleic acid (PNA) conjugates combat antibiotic resistance. These dual-action compounds show enhanced activity against resistant bacterial strains by combining membrane interaction and antisense mechanisms.
Area of Science:
- Microbiology
- Medicinal Chemistry
- Molecular Biology
Background:
- Aminoglycosides (AGs) are crucial antibiotics facing widespread resistance.
- Antimicrobial resistance necessitates novel therapeutic strategies.
Purpose of the Study:
- To develop and evaluate novel aminoglycoside-peptide nucleic acid (PNA) conjugates.
- To overcome resistance in bacterial strains against aminoglycosides.
Main Methods:
- Synthesis of neomycin (NEO) and amikacin (AMK) conjugated with PNA oligomers via click chemistry.
- Assessment of antibacterial activity against resistant strains.
- Mechanism of action studies including membrane permeabilization and transporter dependence.
Main Results:
- AG-PNA conjugates demonstrated superior activity against AG-resistant bacteria compared to parent AGs or mixtures.
- The NEO-PNA conjugate showed efficacy against neomycin-resistant Salmonella Typhimurium LT2 at 8 μM.
- Antisense mechanism confirmed through control experiments; inner membrane identified as a key barrier.
Conclusions:
- AG-PNA conjugates offer a promising dual-action strategy against aminoglycoside-resistant bacteria.
- This approach combines membrane interaction with antisense activity to restore antibiotic efficacy.
- Further development of AG-PNA conjugates could address the challenge of antimicrobial resistance.
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