ArticleProceedings of the National Academy of Sciences of the United States of America2013
Antibacterial drug leads targeting isoprenoid biosynthesis.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 57 papers.
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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.
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Who cites it
57 citing papers in PubMed, 108 citations in OpenAlex.
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- Investigating the Antimicrobial Potential of 560 Compounds from the Pandemic Response Box and COVID Box against Resistant Gram-Negative Bacteria.Antibiotics (Basel, Switzerland) · 2024Article
- Synthesis and structure-activity relationship of novel thiazole aminoguanidines against MRSA andRSC medicinal chemistry · 2024Article
- Lead generation of UPPS inhibitors targeting MRSA: Using 3D-QSAR pharmacophore modeling, virtual screening, molecular docking, and molecular dynamic simulations.BMC chemistry · 2024Article
- Optimization of oil yield of Pelargonium graveolens L'Hér using Box-Behnken design in relation to its antimicrobial activity and in silico study.Scientific reports · 2023Article
- Small Molecules Incorporating Privileged Amidine Moiety as Potential Hits Combating Antibiotic-Resistant Bacteria.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Escaping ESKAPE resistance:Royal Society open science · 2023Article
- Investigations into the antibacterial effects and potential mechanism of gambogic acid and neogambogic acid.Frontiers in microbiology · 2022Article
- Applications of machine learning in computer-aided drug discovery.QRB discovery · 2022Review
- β-Lactams against the Fortress of the Gram-PositiveChemical reviews · 2021Review
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- Identification of Novel Cyclin A2 Binding Site and Nanomolar Inhibitors of Cyclin A2-CDK2 Complex.Current computer-aided drug design · 2021Article
- Immuno-antibiotics: targeting microbial metabolic pathways sensed by unconventional T cells.Immunotherapy advances · 2021Review
- Investigations into the Antibacterial Mechanism of Action of Viridicatumtoxins.ACS infectious diseases · 2020Article
- Cocktailed fragment screening by X-ray crystallography of the antibacterial target undecaprenyl pyrophosphate synthase from Acinetobacter baumannii.Acta crystallographica. Section F, Structural biology communications · 2020Article
- A computational study of the molecular basis of antibiotic resistance in a DXR mutant.Journal of computer-aided molecular design · 2019Article
Corrections and comments
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Authors and funding
18 authors at 4 institutions in 2 countries.
Funding
Abstract
With the rise in resistance to antibiotics such as methicillin, there is a need for new drugs. We report here the discovery and X-ray crystallographic structures of 10 chemically diverse compounds (benzoic, diketo, and phosphonic acids, as well as a bisamidine and a bisamine) that inhibit bacterial undecaprenyl diphosphate synthase, an essential enzyme involved in cell wall biosynthesis. The inhibitors bind to one or more of the four undecaprenyl diphosphate synthase inhibitor binding sites identified previously, with the most active leads binding to site 4, outside the catalytic center. The most potent leads are active against Staphylococcus aureus [minimal inhibitory concentration (MIC)(90) ∼0.25 µg/mL], and one potently synergizes with methicillin (fractional inhibitory concentration index = 0.25) and is protective in a mouse infection model. These results provide numerous leads for antibacterial development and open up the possibility of restoring sensitivity to drugs such as methicillin, using combination therapies.
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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.