What question did this study set out to answer?

Determine whether chemical modifications at the 4'-position of aminoglycosides can improve selectivity for bacterial ribosomes over eukaryotic mitochondrial and cytosolic ribosomes.

January 28, 2014Nature CommunicationsOpen Access

4′-O-substitutions determine selectivity of aminoglycoside antibiotics

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Determine whether chemical modifications at the 4'-position of aminoglycosides can improve selectivity for bacterial ribosomes over eukaryotic mitochondrial and cytosolic ribosomes.
Synthesized a series of 4',6'-O-acetal and 4'-O-ether modifications on glucopyranosyl ring I of 2-deoxystreptamine aminoglycosides.
Assessed compound interactions against ribosomes engineered with single point mutations in the ribosomal drug-binding pocket.
Evaluated functional inhibition and antibacterial activity against bacterial, eukaryotic cytosolic, and eukaryotic mitochondrial ribosomal targets.
Synthesized 4'-O-substituted aminoglycosides displayed poor binding interaction with the drug-binding pockets of eukaryotic cytosolic and mitochondrial ribosomes.
The modified compounds retained potent inhibitory activity against bacterial ribosomes and maintained effective antibacterial activity.

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Implication

Biochemical study reveals modified aminoglycosides selectively inhibit bacterial ribosomes over eukaryotic targets, indicating potential for less toxic antibiotic therapies.

Cite This Study

Perez‐Fernandez et al. (2014) studied this question.

synapsesocial.com/papers/6aa906d525280296cf29a244 https://doi.org/10.1038/ncomms4112

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Implication

Biochemical study reveals modified aminoglycosides selectively inhibit bacterial ribosomes over eukaryotic targets, indicating potential for less toxic antibiotic therapies.

4′-O-substitutions determine selectivity of aminoglycoside antibiotics

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Discussion

Implication

Cite This Study

4′-O-substitutions determine selectivity of aminoglycoside antibiotics

Key Points

Discussion

Implication

Cite This Study

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