Works (5)

Updated: July 5th, 2023 15:43

2017 journal article

Targeting of Streptococcus mutans Biofilms by a Novel Small Molecule Prevents Dental Caries and Preserves the Oral Microbiome

JOURNAL OF DENTAL RESEARCH, 96(7), 807–814.

By: S. Garcia*, M. Blackledge n, S. Michalek*, L. Su*, T. Ptacek*, P. Eipers*, C. Morrow*, E. Lefkowitz*, C. Melander n, H. Wu*

author keywords: microbiota; rats; dental enamel; microscopy; bacteria; microbial ecology
MeSH headings : Animals; Biofilms / drug effects; Dental Caries / prevention & control; Dental Enamel / drug effects; Imidazoles / pharmacology; Microbiota / drug effects; Microscopy, Confocal; Polymerase Chain Reaction; Rats; Streptococcus gordonii / drug effects; Streptococcus mutans / drug effects; Streptococcus sanguis / drug effects
TL;DR: It is demonstrated that selective targeting of S. mutans biofilms by 3F1 was able to effectively reduce dental caries in vivo without affecting the overall oral microbiota shaped by the intake of dietary sugars, suggesting that the pathogenic biofilm-specific treatment is a viable strategy for disease prevention. (via Semantic Scholar)
UN Sustainable Development Goal Categories
Source: Web Of Science
Added: August 6, 2018

2015 journal article

Membrane-Permeabilizing Activity of Reverse-Amide 2-Aminoimidazole Antibiofilm Agents Against Acinetobacter baumannii

CURRENT DRUG DELIVERY, 12(2), 223–230.

By: S. Stowe*, R. Thompson*, L. Peng*, Z. Su*, M. Blackledge*, G. Draughn, W. Coe, E. Johannes* ...

author keywords: 2-aminoimidazole; Acinetobacter baumannii; biofilm; membrane permeabilization; reverse amide; SEM
MeSH headings : Acinetobacter baumannii / drug effects; Amides / chemistry; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Cell Membrane Permeability / drug effects; Cells, Cultured; Cross Infection; Imidazoles / chemistry; Imidazoles / pharmacology; Microbial Sensitivity Tests
TL;DR: A model is proposed that describes how the structure of RA-2AI allows it to insert itself into and disrupt the fluidity of the membrane, creating an opportunity for increased molecular permeability. (via Semantic Scholar)
UN Sustainable Development Goal Categories
Source: Web Of Science
Added: August 6, 2018

2013 journal article

Biologically inspired strategies for combating bacterial biofilms

CURRENT OPINION IN PHARMACOLOGY, 13(5), 699–706.

By: M. Blackledge n, R. Worthington n & C. Melander n

MeSH headings : Animals; Anti-Bacterial Agents / pharmacology; Anti-Bacterial Agents / therapeutic use; Bacterial Infections / drug therapy; Bacterial Infections / metabolism; Bacterial Physiological Phenomena / drug effects; Biofilms / drug effects; Humans; Quorum Sensing / drug effects; Signal Transduction / drug effects
TL;DR: Small molecule interference with bacterial communication and signaling pathways, including quorum sensing and two-component signal transduction systems are focused on, focusing firstly on enzymatic approaches to the degradation of extracellular matrix components to effect biofilm dispersal. (via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being (Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018

2013 journal article

Programmable DNA-binding small molecules

BIOORGANIC & MEDICINAL CHEMISTRY, 21(20), 6101–6114.

By: M. Blackledge n & C. Melander n

author keywords: Polyamide; Transcription; Minor groove; DNA binding
MeSH headings : Animals; DNA / chemistry; DNA / drug effects; DNA / genetics; Gene Expression / drug effects; Humans; Imidazoles / chemistry; Imidazoles / pharmacology; Pyrroles / chemistry; Pyrroles / pharmacology
TL;DR: A brief history of early seminal developments in the field is presented and recent reports of the utility of polyamides as both genetic modulators and molecular probes are highlighted. (via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being (Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018

2013 review

Small-molecule inhibition of bacterial two-component systems to combat antibiotic resistance and virulence

[Review of ]. FUTURE MEDICINAL CHEMISTRY, 5(11), 1265–1284.

By: R. Worthington n, M. Blackledge n & C. Melander n

MeSH headings : Bacteria / metabolism; Bacteria / pathogenicity; Bacterial Infections / drug therapy; Bacterial Proteins / antagonists & inhibitors; Bacterial Proteins / metabolism; Biofilms / drug effects; Drug Resistance, Multiple, Bacterial / drug effects; Histidine Kinase; Humans; Protein Kinases / chemistry; Protein Kinases / metabolism; Signal Transduction / drug effects; Small Molecule Libraries / chemistry; Small Molecule Libraries / pharmacology; Small Molecule Libraries / therapeutic use; Virulence / drug effects
TL;DR: An overview of TCS that are potential targets for such a strategy, small-molecules inhibitors of T CS identified to date are described, and assays for the identification of novel inhibitors are discussed. (via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being (Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018

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