ArticleBioorganic & medicinal chemistry2011
Inhibition of LuxS by S-ribosylhomocysteine analogues containing a [4-aza]ribose ring.
Article in Bioorganic & medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 40 citations in OpenAlex.
- Quorum sensing in bacteria: insights into communication and inhibition strategies-a review.Archives of microbiology · 2026Review
- Predicting target-ligand interactions with graph convolutional networks for interpretable pharmaceutical discovery.Scientific reports · 2022Article
- 5-Fluorouracil blocks quorum-sensing of biofilm-embedded methicillin-resistant Staphylococcus aureus in mice.Nucleic acids research · 2021Article
- Exploring interfacial dynamics in homodimericRSC advances · 2021Article
- Regulatory Mechanisms of the LuxS/AI-2 System and Bacterial Resistance.Antimicrobial agents and chemotherapy · 2019Review
- Saline Environments as a Source of Potential Quorum Sensing Disruptors to Control Bacterial Infections: A Review.Marine drugs · 2019Review
- Design, Synthesis and Biological Evaluation of Isoxazole-Based CK1 Inhibitors Modified with Chiral Pyrrolidine Scaffolds.Molecules (Basel, Switzerland) · 2019Article
- Quorum sensing in thermophiles: prevalence of autoinducer-2 system.BMC microbiology · 2018Article
- Designer cells programming quorum-sensing interference with microbes.Nature communications · 2018Article
- Interference With Quorum-Sensing Signal Biosynthesis as a Promising Therapeutic Strategy Against Multidrug-Resistant Pathogens.Frontiers in cellular and infection microbiology · 2018Review
- Reduction of sugar lactones to hemiacetals with lithium triethylborohydride.Carbohydrate research · 2016Article
- S-Ribosylhomocysteine analogs containing a [4-thio]ribose ring.Carbohydrate research · 2015Article
- Screening of Actinobacillus pleuropneumoniae LuxS inhibitors.Current microbiology · 2013Article
- Small molecule inhibitors of AI-2 signaling in bacteria: state-of-the-art and future perspectives for anti-quorum sensing agents.International journal of molecular sciences · 2013Article
- Exploiting quorum sensing to confuse bacterial pathogens.Microbiology and molecular biology reviews : MMBR · 2013Review
- Substituted lactam and cyclic azahemiacetals modulate Pseudomonas aeruginosa quorum sensing.Bioorganic & medicinal chemistry · 2011Article
- Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
LuxS (S-ribosylhomocysteinase) catalyzes the cleavage of the thioether linkage of S-ribosylhomocysteine (SRH) to produce homocysteine and 4,5-dihydroxy-2,3-pentanedione (DPD), the precursor to a small signaling molecule that mediates interspecies bacterial communication called autoinducer 2 (AI-2). Inhibitors of LuxS should interfere with bacterial interspecies communication and potentially provide a novel class of antibacterial agents. In this work, SRH analogues containing substitution of a nitrogen atom for the endocyclic oxygen as well as various deoxyriboses were synthesized and evaluated for LuxS inhibition. Two of the [4-aza]SRH analogues showed modest competitive inhibition (K(I) ∼40 μM), while most of the others were inactive. One compound that contains a hemiaminal moiety exhibited time-dependent inhibition, consistent with enzyme-catalyzed ring opening and conversion into a more potent species (K(I)(∗)=3.5 μM). The structure-activity relationship of the designed inhibitors highlights the importance of both the homocysteine and ribose moieties for high-affinity binding to LuxS active site.
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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.