ArticleAntimicrobial agents and chemotherapy2013
Solithromycin inhibition of protein synthesis and ribosome biogenesis in Staphylococcus aureus, Streptococcus pneumoniae, and Haemophilus influenzae.
Article in Antimicrobial agents and chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed.
- Exploring the repurposed role of solithromycin as an antivirulence agent againstFrontiers in microbiology · 2025Article
- Therapeutic applications of carbohydrate-based compounds: a sweet solution for medical advancement.Molecular diversity · 2024Review
- Development of Genetically Encoded Biosensors for Reporting the Methyltransferase-Dependent Biosynthesis of Semisynthetic Macrolide Antibiotics.ACS synthetic biology · 2021Article
- The frontiers of addressing antibiotic resistance in Neisseria gonorrhoeae.Translational research : the journal of laboratory and clinical medicine · 2020Review
- Antibiotics targeting bacterial ribosomal subunit biogenesis.The Journal of antimicrobial chemotherapy · 2020Review
- Population Pharmacokinetics and Safety of Solithromycin following Intravenous and Oral Administration in Infants, Children, and Adolescents.Antimicrobial agents and chemotherapy · 2018Article
- Ribosome maturation by the endoribonuclease YbeY stabilizes a type 3 secretion system transcript required for virulence of enterohemorrhagicThe Journal of biological chemistry · 2018Article
- Development of an Adult Physiologically Based Pharmacokinetic Model of Solithromycin in Plasma and Epithelial Lining Fluid.CPT: pharmacometrics & systems pharmacology · 2017Article
- Article
- The Human Ureaplasma Species as Causative Agents of Chorioamnionitis.Clinical microbiology reviews · 2017Review
- Spotlight on solithromycin in the treatment of community-acquired bacterial pneumonia: design, development, and potential place in therapy.Drug design, development and therapy · 2017Review
- Antibiotics in the clinical pipeline at the end of 2015.The Journal of antibiotics · 2017Review
- Solithromycin: A Novel Fluoroketolide for the Treatment of Community-Acquired Bacterial Pneumonia.Drugs · 2016Review
- Efficacy of Solithromycin (CEM-101) for Experimental Otitis Media Caused by Nontypeable Haemophilus influenzae and Streptococcus pneumoniae.Antimicrobial agents and chemotherapy · 2016Article
- Results from the Solithromycin International Surveillance Program (2014).Antimicrobial agents and chemotherapy · 2016Article
- A New, Potent, and Placenta-Permeable Macrolide Antibiotic, Solithromycin, for the Prevention and Treatment of Bacterial Infections in Pregnancy.Frontiers in immunology · 2016Review
- Progress in the discovery of treatments for C. difficile infection: A clinical and medicinal chemistry review.Current topics in medicinal chemistry · 2014Review
- Maternal administration of solithromycin, a new, potent, broad-spectrum fluoroketolide antibiotic, achieves fetal and intra-amniotic antimicrobial protection in a pregnant sheep model.Antimicrobial agents and chemotherapy · 2014Article
- Investigational antimicrobial agents of 2013.Clinical microbiology reviews · 2013Review
Corrections and comments
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The continuing increase in antibiotic-resistant microorganisms is driving the search for new antibiotic targets and improved antimicrobial agents. Ketolides are semisynthetic derivatives of macrolide antibiotics, which are effective against certain resistant organisms. Solithromycin (CEM-101) is a novel fluoroketolide with improved antimicrobial effectiveness. This compound binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis. Like other ketolides, it should impair bacterial ribosomal subunit formation. This mechanism of action was examined in strains of Streptococcus pneumoniae, Staphylococcus aureus, and Haemophilus influenzae. The mean 50% inhibitory concentrations (IC50s) for solithromycin inhibition of cell viability, protein synthesis, and growth rate were 7.5, 40, and 125 ng/ml for Streptococcus pneumoniae, Staphylococcus aureus, and Haemophilus influenzae, respectively. The net formation of the 50S subunit was reduced in all three organisms, with IC50s similar to those given above. The rates of 50S subunit formation measured by a pulse-chase labeling procedure were reduced by 75% in cells growing at the IC50 of solithromycin. Turnover of 23S rRNA was stimulated by solithromycin as well. Solithromycin was found to be a particularly effective antimicrobial agent, with IC50s comparable to those of telithromycin and significantly better than those of azithromycin and clarithromycin in these three microorganisms.
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