ArticleAntimicrobial agents and chemotherapy2016
Molecule Targeting Glucosyltransferase Inhibits Streptococcus mutans Biofilm Formation and Virulence.
Article in Antimicrobial agents and chemotherapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 95 papers.
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Who cites it
95 citing papers in PubMed, 170 citations in OpenAlex.
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- Characterization and Evaluation of Lactic Acid Bacteria from Feline Milk for Probiotic Properties.Animals : an open access journal from MDPI · 2025Article
- Advances and challenges in drug design against dental caries: Application ofJournal of pharmaceutical analysis · 2025Review
- Evaluation of the effect of different infant formulas on Streptococcus mutans biofilm formation: an in-vitro study.The Saudi dental journal · 2025Article
- A Pyrroloquinazoline Analogue Regulated Streptococcus mutans and Streptococcus sanguinis Dual-Species Biofilms.International dental journal · 2025Article
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- Quinoxalines in Oral Health: From Antimicrobials to Biomaterials.Mini reviews in medicinal chemistry · 2025Review
- Computational-aided drug design strategies for drug discovery and development against oral diseases.Frontiers in pharmacology · 2025Review
- Article
35 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
11 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Dental plaque biofilms are responsible for numerous chronic oral infections and cause a severe health burden. Many of these infections cannot be eliminated, as the bacteria in the biofilms are resistant to the host's immune defenses and antibiotics. There is a critical need to develop new strategies to control biofilm-based infections. Biofilm formation in Streptococcus mutans is promoted by major virulence factors known as glucosyltransferases (Gtfs), which synthesize adhesive extracellular polysaccharides (EPS). The current study was designed to identify novel molecules that target Gtfs, thereby inhibiting S. mutans biofilm formation and having the potential to prevent dental caries. Structure-based virtual screening of approximately 150,000 commercially available compounds against the crystal structure of the glucosyltransferase domain of the GtfC protein from S. mutans resulted in the identification of a quinoxaline derivative, 2-(4-methoxyphenyl)-N-(3-{[2-(4-methoxyphenyl)ethyl]imino}-1,4-dihydro-2-quinoxalinylidene)ethanamine, as a potential Gtf inhibitor. In vitro assays showed that the compound was capable of inhibiting EPS synthesis and biofilm formation in S. mutans by selectively antagonizing Gtfs instead of by killing the bacteria directly. Moreover, the in vivo anti-caries efficacy of the compound was evaluated in a rat model. We found that the compound significantly reduced the incidence and severity of smooth and sulcal-surface caries in vivo with a concomitant reduction in the percentage of S. mutans in the animals' dental plaque (P < 0.05). Taken together, these results represent the first description of a compound that targets Gtfs and that has the capacity to inhibit biofilm formation and the cariogenicity of S. mutans.
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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.