ArticleJournal of biomolecular screening2013
Identification of a small-molecule inhibitor of bacterial AraC family activators.
Article in Journal of biomolecular screening, 2013. 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, 25 citations in OpenAlex.
- Targeting bacterial transcription factors for infection control: opportunities and challenges.Transcription · 2025Review
- β-Lactam potentiators to re-sensitize resistant pathogens: Discovery, development, clinical use and the way forward.Frontiers in microbiology · 2022Review
- A high-throughput system to identify inhibitors ofProceedings of the National Academy of Sciences of the United States of America · 2019Article
- Zika virus outbreak: a review of neurological complications, diagnosis, and treatment options.Journal of neurovirology · 2018Review
- The Multifaceted Activity of the VirF Regulatory Protein in theFrontiers in molecular biosciences · 2016Review
- Role of Escherichia coli in Biofuel Production.Microbiology insights · 2016Review
- Mechanism of Action and Initial, In Vitro SAR of an Inhibitor of the Shigella flexneri Virulence Regulator VirF.PloS one · 2015Article
- 3-Substituted Biquinolinium Inhibitors of AraC Family Transcriptional Activator VirF fromRSC advances · 2014Article
- Small-molecule inhibitor of the Shigella flexneri master virulence regulator VirF.Infection and immunity · 2013Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Protein members of the AraC family of bacterial transcriptional activators have great promise as targets for the development of novel antibacterial agents. Here, we describe an in vivo high-throughput screen to identify inhibitors of the AraC family activator protein RhaS. The screen used two Escherichia coli reporter fusions: one to identify potential RhaS inhibitors and a second to eliminate nonspecific inhibitors from consideration. One compound with excellent selectivity, OSSL_051168, was chosen for further study. OSSL_051168 inhibited in vivo transcription activation by the RhaS DNA-binding domain to the same extent as the full-length protein, indicating that this domain was the target of its inhibition. Growth curves showed that OSSL_051168 did not affect bacterial cell growth at the concentrations used in this study. In vitro DNA-binding assays with purified protein suggest that OSSL_051168 inhibits DNA binding by RhaS. In addition, we found that it inhibits DNA binding by a second AraC family protein, RhaR, which shares 30% amino acid identity with RhaS. OSSL_051168 did not have a significant impact on DNA binding by the non-AraC family proteins CRP and LacI, suggesting that the inhibition is likely specific for RhaS, RhaR, and possibly additional AraC family activator proteins.
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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.