Retapamulin inhibited protein biosynthesis and cell viability in methicillin-sensitive and methicillin-resistant Staphylococcus aureus organisms. A specific inhibitory effect on 50S ribosomal subunit formation was also found. Pulse-chase labeling experiments confirmed the specific inhibition of 50S subunit biogenesis. Turnover of 23S rRNA was found, with no effect on 16S rRNA amounts.
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http://dx.doi.org/10.1128/AAC.00475-07 | DOI Listing |
J Med Chem
January 2025
Xi'an Key Laboratory for Antiviral and Antimicrobial-Resistant Bacteria Therapeutics Research, Xi'an 710021, China.
Multidrug-resistant (MDR) bacteria pose a global health threat, underscoring the need for new antibiotics. Lefamulin, the first novel-mechanism antibiotic approved by the FDA in decades, showcases pleuromutilins' promise due to low mutation frequency. However, their clinical use is limited by poor pharmacokinetics and organ toxicity.
View Article and Find Full Text PDFVet Med Int
January 2025
Department of Science and Technology, Virology and Vaccine Research Program, Industrial Technology Development Institute, Bicutan, Taguig 1634, Philippines.
African swine fever (ASF), caused by African swine fever virus (ASFV), is a highly contagious disease with devastating effects on the global pig industry. This warrants the development of effective control strategies, such as vaccines. However, previously developed inactivated vaccines have proven ineffective, while live-attenuated vaccines carry inherent safety risks.
View Article and Find Full Text PDFNat Commun
January 2025
Institute of Bioanalytical Chemistry, Faculty of Chemistry and Mineralogy, Universität Leipzig, Leipzig, Germany.
The proline-rich antimicrobial designer peptide Api137 inhibits protein expression in bacteria by binding simultaneously to the ribosomal polypeptide exit tunnel and the release factor (RF), depleting the cellular RF pool and leading to ribosomal arrest at stop codons. This study investigates the additional effect of Api137 on the assembly of ribosomes using an Escherichia coli reporter strain expressing one ribosomal protein per 30S and 50S subunit tagged with mCherry and EGFP, respectively. Separation of cellular extracts derived from cells exposed to Api137 in a sucrose gradient reveals elevated levels of partially assembled and not fully matured precursors of the 50S subunit (pre-50S).
View Article and Find Full Text PDFJ Biomol Struct Dyn
January 2025
Department of Studies in Physics, University of Mysore, Mysuru, India.
Int J Mol Sci
November 2024
Departamento de Biotecnología, Universidad Autónoma Metropolitana Unidad Iztapalapa, Av. San Rafael Atlixco 186, Col. Vicentina, Mexico City 09340, Mexico.
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