Polymer vesicles for the delivery of inhibitors of cariogenic biofilm.

Objectives: The goal of this study is to develop a novel drug delivery platform for the pH-responsive delivery of biofilm inhibitors as a potential avenue to prevent and treat dental caries.

Methods: Biofilm and growth inhibition assays were performed in polystyrene microtiter 96-well plates. Docking analysis was performed using the reported GtfB + HA5 co-crystal structure (PDB code: 8fg8) in SeeSAR 13.

Therapeutic targeting of voltage-gated sodium channel Na1.7 for cancer metastasis.

This review focuses on the expression and function of voltage-gated sodium channel subtype Na1.7 in various cancers and explores its impact on the metastasis driving cell functions such as proliferation, migration, and invasiveness. An overview of its structural characteristics, drug binding sites, inhibitors and their likely mechanisms of action are presented.

Voltage-Gated Sodium Channel Na1.7 Inhibitors with Potent Anticancer Activities in Medullary Thyroid Cancer Cells.

Our results from quantitative RT-PCR, Western blotting, immunohistochemistry, and the tissue microarray of medullary thyroid cancer (MTC) cell lines and patient specimens confirm that VGSC subtype Na1.7 is uniquely expressed in aggressive MTC and not expressed in normal thyroid cells and tissues. We establish the druggability of Na1.

Hydrogel-Encapsulated Biofilm Inhibitors Abrogate the Cariogenic Activity of .

We designed and synthesized analogues of a previously identified biofilm inhibitor to improve solubility, retain inhibitory activities, and to facilitate encapsulation into pH-responsive hydrogel microparticles. The optimized lead compound showed improved solubility of 120.09 μg/mL, inhibited biofilm with an IC value of 6.

Voltage-Gated Sodium Channel Na1.5 Controls NHE-1-Dependent Invasive Properties in Colon Cancer Cells.

Colorectal cancer (CRC) is the second leading cause of death worldwide, with 0.9 million deaths per year. The metastatic stage of the disease is identified in about 20% of cases at the first diagnosis and is associated with low patient-survival rates.

Pharmacological and nutritional targeting of voltage-gated sodium channels in the treatment of cancers.

Voltage-gated sodium (Na) channels, initially characterized in excitable cells, have been shown to be aberrantly expressed in non-excitable cancer tissues and cells from epithelial origins such as in breast, lung, prostate, colon, and cervix, whereas they are not expressed in cognate non-cancer tissues. Their activity was demonstrated to promote aggressive and invasive potencies of cancer cells, both and , whereas their deregulated expression in cancer tissues has been associated with metastatic progression and cancer-related death. This review proposes Na channels as pharmacological targets for anticancer treatments providing opportunities for repurposing existing Na-inhibitors or developing new pharmacological and nutritional interventions.

Discovery of Potent Inhibitors of Biofilm with Antivirulence Activity.

Dental caries is a bacterial infectious disease characterized by demineralization of the tooth enamel. Treatment of this disease with conventional antibiotics is largely ineffective as the cariogenic bacteria form tenacious biofilms that are resistant to such treatments. The main etiological agent for dental caries is the bacterium .