ArticleToxicon : official journal of the International Society on Toxinology2010
The identification and biochemical characterization of drug-like compounds that inhibit botulinum neurotoxin serotype A endopeptidase activity.
Article in Toxicon : official journal of the International Society on Toxinology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 24 citations in OpenAlex.
- Clostridial Neurotoxins: Structure, Function and Implications to Other Bacterial Toxins.Microorganisms · 2021Review
- Natural Compounds and Their Analogues as Potent Antidotes against the Most Poisonous Bacterial Toxin.Applied and environmental microbiology · 2018Article
- A Novel Surface Plasmon Resonance Biosensor for the Rapid Detection of Botulinum Neurotoxins.Biosensors · 2017Article
- Selection of RNA Aptamers Against Botulinum Neurotoxin Type A Light Chain Through a Non-Radioactive Approach.Applied biochemistry and biotechnology · 2016Article
- Effect of botulinum neurotoxin type A (BoNTA) on the morphology and viability of 3T3 murine fibroblasts.International journal of clinical and experimental pathology · 2015Article
- Cleavage of SNAP25 and its shorter versions by the protease domain of serotype A botulinum neurotoxin.PloS one · 2014Article
- Paclitaxel is an inhibitor and its boron dipyrromethene derivative is a fluorescent recognition agent for botulinum neurotoxin subtype A.Journal of medicinal chemistry · 2013Article
- Small-molecule quinolinol inhibitor identified provides protection against BoNT/A in mice.PloS one · 2012Article
- High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.Antiviral research · 2011Article
- In vitro selection of RNA aptamers that inhibit the activity of type A botulinum neurotoxin.Biochemical and biophysical research communications · 2010Article
- Small molecules showing significant protection of mice against botulinum neurotoxin serotype A.PloS one · 2010Article
- Botulinum neurotoxin A protease: discovery of natural product exosite inhibitors.Journal of the American Chemical Society · 2010Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
A robust, high-throughput, two-tiered assay for screening small molecule inhibitors against botulinum neurotoxin serotype A was developed and employed to screen 16,544 compounds. Thirty-four compounds were identified as potent hits employing the first-tier assay. Subsequently, nine were confirmed as actives by our second-tier confirmatory assay. Of these, one displayed potent inhibitory efficacy, possessing an IC(50)=16 microM (+/-1.6 microM) in our in vitro assay. This inhibitor (0831-1035) is highly water-soluble, and possesses an IC(50)=47 microM (+/-7.0 microM) in our primary cell culture assay (with virtually no cytotoxicity up to 500 microM), suggesting that this inhibitor is a good candidate for further development as a therapeutic countermeasure to treat botulism resulting from botulinum neurotoxin serotype A intoxication. An enzyme kinetics study indicated that this inhibitor exhibits mixed non-competitive inhibition, with a K(I)=9 microM.
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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.