ArticleAntimicrobial agents and chemotherapy2008
R chi-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance.
Article in Antimicrobial agents and chemotherapy, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
28 citing papers in PubMed, 72 citations in OpenAlex.
- Structural modification of oxazolidinone antibiotics alters nascent peptide stalling preference and peptide trajectory through the ribosome.bioRxiv : the preprint server for biology · 2026Article
- Hybrid Antibiotics Targeting the Bacterial Ribosome.ACS central science · 2025Article
- A Comprehensive Overview of the Antibiotics Approved in the Last Two Decades: Retrospects and Prospects.Molecules (Basel, Switzerland) · 2023Review
- Selective toxicity of antibacterial agents-still a valid concept or do we miss chances and ignore risks?Infection · 2021Review
- Antibiotics targeting bacterial ribosomal subunit biogenesis.The Journal of antimicrobial chemotherapy · 2020Review
- Minocycline modulates NFκB phosphorylation and enhances antimicrobial activity against Staphylococcus aureus in mesenchymal stromal/stem cells.Stem cell research & therapy · 2017Article
- Minocycline enhances the mesenchymal stromal/stem cell pro-healing phenotype in triple antimicrobial-loaded hydrogels.Acta biomaterialia · 2017Article
- Antibiotics in the clinical pipeline at the end of 2015.The Journal of antibiotics · 2017Review
- Ribosomal frameshifting and transcriptional slippage: From genetic steganography and cryptography to adventitious use.Nucleic acids research · 2016Review
- Article
- Targeting Antibiotic Resistance.Angewandte Chemie (International ed. in English) · 2016Review
- Complex long-distance effects of mutations that confer linezolid resistance in the large ribosomal subunit.Nucleic acids research · 2015Article
- Article
- An azido-oxazolidinone antibiotic for live bacterial cell imaging and generation of antibiotic variants.Bioorganic & medicinal chemistry · 2014Article
- Pipeline of Known Chemical Classes of Antibiotics.Antibiotics (Basel, Switzerland) · 2013Review
- Advances in MRSA drug discovery: where are we and where do we need to be?Expert opinion on drug discovery · 2013Review
- The antibiotic thermorubin inhibits protein synthesis by binding to inter-subunit bridge B2a of the ribosome.Journal of molecular biology · 2012Article
- The chemistry of peptidyltransferase center-targeted antibiotics: enzymatic resistance and approaches to countering resistance.ACS chemical biology · 2012Review
- Current updates on oxazolidinone and its significance.International journal of medicinal chemistry · 2012Review
- Structure-activity relationships of diverse oxazolidinones for linezolid-resistant Staphylococcus aureus strains possessing the cfr methyltransferase gene or ribosomal mutations.Antimicrobial agents and chemotherapy · 2010Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
New and improved antibiotics are urgently needed to combat the ever-increasing number of multidrug-resistant bacteria. In this study, we characterized several members of a new oxazolidinone family, R chi-01. This antibiotic family is distinguished by having in vitro and in vivo activity against hospital-acquired, as well as community-acquired, pathogens. We compared the 50S ribosome binding affinity of this family to that of the only marketed oxazolidinone antibiotic, linezolid, using chloramphenicol and puromycin competition binding assays. The competition assays demonstrated that several members of the R chi-01 family displace, more effectively than linezolid, compounds known to bind to the ribosomal A site. We also monitored binding by assessing whether R chi-01 compounds protect U2585 (Escherichia coli numbering), a nucleotide that influences peptide bond formation and peptide release, from chemical modification by carbodiimide. The R chi-01 oxazolidinones were able to inhibit translation of ribosomes isolated from linezolid-resistant Staphylococcus aureus at submicromolar concentrations. This improved binding corresponds to greater antibacterial activity against linezolid-resistant enterococci. Consistent with their ribosomal A-site targeting and greater potency, the R chi-01 compounds promote nonsense suppression and frameshifting to a greater extent than linezolid. Importantly, the gain in potency does not impact prokaryotic specificity as, like linezolid, the members of the R chi-01 family show translation 50% inhibitory concentrations that are at least 100-fold higher for eukaryotic than for prokaryotic ribosomes. This new family of oxazolidinones distinguishes itself from linezolid by having greater intrinsic activity against linezolid-resistant isolates and may therefore offer clinicians an alternative to overcome linezolid resistance. A member of the R chi-01 family of compounds is currently undergoing clinical trials.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.