ArticleBioorganic & medicinal chemistry2009
Structure-activity relationship studies of a novel series of anthrax lethal factor inhibitors.
Article in Bioorganic & medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 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
9 citing papers in PubMed, 22 citations in OpenAlex.
- Targeting Metalloenzymes for Therapeutic Intervention.Chemical reviews · 2019Review
- Design and use of a novel substrate for simple, rapid, and specific early detection of anthrax infection.PloS one · 2018Article
- Highly predictive support vector machine (SVM) models for anthrax toxin lethal factor (LF) inhibitors.Journal of molecular graphics & modelling · 2016Article
- Inhibitors of the Metalloproteinase Anthrax Lethal Factor.Current topics in medicinal chemistry · 2016Review
- Development of a comprehensive, validated pharmacophore hypothesis for anthrax toxin lethal factor (LF) inhibitors using genetic algorithms, Pareto scoring, and structural biology.Journal of chemical information and modeling · 2012Article
- Microbial and fungal protease inhibitors--current and potential applications.Applied microbiology and biotechnology · 2012Review
- N-(Prop-2-yn-1-yl)-1,3-benzothia-zol-2-amine.Acta crystallographica. Section E, Structure reports online · 2011Article
- Targeting metalloproteins by fragment-based lead discovery.Chemical biology & drug design · 2011Article
- Identifying chelators for metalloprotein inhibitors using a fragment-based approach.Journal of medicinal chemistry · 2011Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 3 institutions in 1 country.
Funding
Abstract
We report on the identification of a novel small molecule inhibitor of anthrax lethal factor using a high-throughput screening approach. Guided by molecular docking studies, we carried out structure-activity relationship (SAR) studies and evaluated activity and selectivity of most promising compounds in in vitro enzyme inhibition assays and cellular assays. Selected compounds were further analyzed for their in vitro ADME properties, which allowed us to select two compounds for further preliminary in vivo efficacy studies. The data provided represents the basis for further pharmacology and medicinal chemistry optimizations that could result in novel anti-anthrax therapies.
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What OpenQuestion holds
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.