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Updated: Aug 23, 2026

Biosensor for Detection of Antibiotic Resistant Staphylococcus Bacteria
Published on: May 8, 2013
Macrolide resistance in Staphylococcus aureus: inducers of macrolide resistance
Abstract:
Several macrolide-, lincosamide-, and streptogramin B-type (MLS) antibiotics were tested as inducers of erythromycin A (EM)-resistant [(14)C]leucine incorporation. Only 14-membered-ring macrolides having a glycosidically linked 6-deoxy sugar at the C-3 position of the lactone ring and the structurally dissimilar lincosamide, celesticetin, showed inducer activity. Modifications of EM at the C-4'' position of cladinose can apparently destroy the inducer property but do not affect the inhibitory properties of the antibiotic. The findings clearly show that inducer and inhibitor activities can be dissociated and are consistent with the concept that distinct binding/receptor sites are utilized for inhibition of ribosome function and induction of resistance.
Insights
Certain macrolide antibiotics and celesticetin induce resistance by targeting specific sites. Modifications to erythromycin A (EM) can abolish induction while retaining inhibition, showing distinct mechanisms for these antibiotic effects.
Area of Science:
- Microbiology
- Molecular Biology
- Biochemistry
Background:
- Macrolide-, lincosamide-, and streptogramin B-type (MLS) antibiotics are crucial in treating bacterial infections.
- Understanding the mechanisms of antibiotic resistance, particularly induction of resistance, is vital for developing new therapeutic strategies.
Purpose of the Study:
- To investigate the specific structural requirements of MLS antibiotics for inducing resistance.
- To determine if antibiotic-induced resistance and inhibition share common molecular targets.
Main Methods:
- Testing various MLS antibiotics for their ability to induce [(14)C]leucine incorporation resistant to erythromycin A (EM).
- Analyzing the structure-activity relationship of EM modifications on inducer and inhibitor properties.
Main Results:
- Only 14-membered ring macrolides with a 6-deoxy sugar at C-3 and the lincosamide celesticetin demonstrated inducer activity.
- Modifications at the C-4'' position of EM's cladinose abolished inducer activity but not inhibitory effects.
Conclusions:
- Inducer and inhibitor activities of MLS antibiotics can be dissociated, suggesting different molecular targets.
- Distinct binding sites are likely involved in ribosome inhibition and resistance induction by these antibiotics.
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Development of Antibiotic Resistance
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