ArticleJournal of the American Chemical Society2013
Tuning the moenomycin pharmacophore to enable discovery of bacterial cell wall synthesis inhibitors.
Article in Journal of the American Chemical Society, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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
18 citing papers in PubMed, 46 citations in OpenAlex.
- Carbamate-Bearing Carbohydrates: Natural Occurrence, Pharmacological Relevance, and Chemical Synthesis.ACS omega · 2026Review
- Article
- A Time-Resolved FRET Assay Identifies a Small Molecule that Inhibits the Essential Bacterial Cell Wall Polymerase FtsW.Angewandte Chemie (International ed. in English) · 2023Article
- Article
- Cell Wall Damage Reveals Spatial Flexibility in Peptidoglycan Synthesis and a Nonredundant Role for RodA in Mycobacteria.Journal of bacteriology · 2022Article
- Rational structural modification of the isatin scaffold to develop new and potent antimicrobial agents targeting bacterial peptidoglycan glycosyltransferase.RSC advances · 2021Article
- Peptidoglycan pathways: there are still more!RSC advances · 2019Review
- Gene ssfg_01967 (miaB) for tRNA modification influences morphogenesis and moenomycin biosynthesis in Streptomyces ghanaensis ATCC14672.Microbiology (Reading, England) · 2019Article
- Towards new antibiotics targeting bacterial transglycosylase: Synthesis of a Lipid II analog as stable transition-state mimic inhibitor.Bioorganic & medicinal chemistry letters · 2018Article
- Don't let sleeping dogmas lie: new views of peptidoglycan synthesis and its regulation.Molecular microbiology · 2017Review
- Moenomycin Biosynthesis: Structure and Mechanism of Action of the Prenyltransferase MoeN5.Angewandte Chemie (International ed. in English) · 2016Article
- Glycosyltransferases and Transpeptidases/Penicillin-Binding Proteins: Valuable Targets for New Antibacterials.Antibiotics (Basel, Switzerland) · 2016Review
- Carbohydrate scaffolds as glycosyltransferase inhibitors with in vivo antibacterial activity.Nature communications · 2015Article
- The evolving role of chemical synthesis in antibacterial drug discovery.Angewandte Chemie (International ed. in English) · 2014Review
- Bioactive oligosaccharide natural products.Natural product reports · 2014Review
- Prospects for novel inhibitors of peptidoglycan transglycosylases.Bioorganic chemistry · 2014Review
- Moenomycin resistance mutations in Staphylococcus aureus reduce peptidoglycan chain length and cause aberrant cell division.ACS chemical biology · 2014Article
- Lipoprotein activators stimulate Escherichia coli penicillin-binding proteins by different mechanisms.Journal of the American Chemical Society · 2014Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
New antibiotic drugs need to be identified to address rapidly developing resistance of bacterial pathogens to common antibiotics. The natural antibiotic moenomycin A is the prototype for compounds that bind to bacterial peptidoglycan glycosyltransferases (PGTs) and inhibit cell wall biosynthesis, but it cannot be used as a drug. Here we report the chemoenzymatic synthesis of a fluorescently labeled, truncated analogue of moenomycin based on the minimal pharmacophore. This probe, which has optimized enzyme binding properties compared to moenomycin, was designed to identify low-micromolar inhibitors that bind to conserved features in PGT active sites. We demonstrate its use in displacement assays using PGTs from S. aureus, E. faecalis, and E. coli. 110,000 compounds were screened against S. aureus SgtB, and we identified a non-carbohydrate based compound that binds to all PGTs tested. We also show that the compound inhibits in vitro formation of peptidoglycan chains by several different PGTs. Thus, this assay enables the identification of small molecules that target PGT active sites, and may provide lead compounds for development of new antibiotics.
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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.