Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are allosteric inhibitors that bind to the HIV reverse transcriptase and prevent replication. Indolyl aryl sulfones (IAS) and IAS derivatives have been found to be highly effective against mutant strains of HIV-1 reverse transcriptase. Here, we analyzed molecules designed using aryl sulfone scaffolds paired to cyclic compounds as potential NNRTIs through the computational design and docking of 100 novel NNRTI candidates. Moreover, we explored the specific combinations of functional groups and aryl sulfones that resulted in the NNRTI candidates with the strongest binding affinity while testing all compounds for carcinogenicity. We hypothesized that the combination of an IAS scaffold and pyrimidine would produce the compounds with the best binding affinity. Our hypothesis was correct as the series of molecules with an IAS scaffold and pyrimidine exhibited the best average binding affinity. Additionally, this study found 32 molecules designed in this procedure with higher or equal binding affinities to the previously successful IAS derivative 5-bromo-3-[(3,5-dimethylphenyl)sulfonyl]indole-2-carboxyamide when docked to HIV-1 reverse transcriptase.
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Bacteroides thetaiotaomicron Growth Numbers Are Unchanged in the Presence of Yogurt
Disruptions to the microbiome, specifically the imbalance in the two major phyla, the Firmicutes and the Bacteroidetes, have been linked to the development of obesity. This study explored whether or not Fage plain total 0% Greek yogurt, which contains live and active bacterial cultures belonging to the Firmicute phylum, could decrease the numbers of Bacteroides thetaiotaomicron, an organism found in the human gut that belongs to the Bacteroidetes phylum.
Read More...Manipulation of extracellular matrix mechanical cues to stimulate oligodendrocytes to promote remyelination
Oligodendrocytes are specialized brain cells that can change to cells that produce myelin and protect nerves. This study investigates the capacity for different extracellular matrix cues to induce this effect in culture.
Read More...Investigating the Role of the Novel ESCRT-III Recruitment Factor CCDC11 in HIV Budding: A Potential Target for Antiviral Therapy
Acquired immunodeficiency syndrome (AIDS) is a life-threatening condition caused by the human immunodeficiency virus (HIV). In this work, Takemaru et al explored the role of Coiled-Coil Domain-Containing 11 (CCDC11) in HIV-1 budding. Their results suggest that CCDC11 is critical for efficient HIV-1 budding, potentially indicating CCDC11 a viable target for antiviral therapeutics without major side effects.
Read More...Conversion of Mesenchymal Stem Cells to Cancer-Associated Fibroblasts in a Tumor Microenvironment: An in vitro Study
Mesenchymal stem cells(MSCs) play a role in tumor formation by differentiating into cancer associated fibroblasts (CAFs) which enable metastasis of tumors. The process of conversion of MSCs into CAFs is not clear. In this study, authors tested the hypothesis that cancers cells secrete soluble factors that induce differentiation by culturing bone marrow mesenchymal stem cells in media conditioned by a breast cancer cell line.
Read More...Giving Teens a Voice: Sources of Stress for High School Students
The authors investigate the negative effects stress has on teen mental and physical health. Through a survey, they give Virginia teens a voice in revising the Health and Physical Education curriculum to include a standards of learning (SOL). Notably they identify factors contributing to stress levels including homework level, amount of free and sleep time, parental pressure and family encouragement.
Read More...The Effects of Antioxidants on the Climbing Abilities of Drosophila melanogaster Exposed to Dental Resin
Dental resins can be a source of reactive oxygen species (ROS) which in unruly amounts can be toxic to cellular and overall health. In this report, the authors test whether the consumption of antioxidant rich foods like avocado and asparagus can protect against the effect of dental resin-derived ROS. However, rather than testing humans, they use fruit flies and their climbing abilities as an experimental readout.
Read More...Analysis of complement system gene expression and outcome across the subtypes of glioma
Here the authors sought to better understand glioma, cancer that occurs in the glial cells of the brain with gene expression profile analysis. They considered the expression of complement system genes across the transcriptional and IDH-mutational subtypes of low-grade glioma and glioblastoma. Based on their results of their differential gene expression analysis, they found that outcomes vary across different glioma subtypes, with evidence suggesting that categorization of the transcriptional subtypes could help inform treatment by providing an expectation for treatment responses.
Read More...Differential MERS-CoV response in different cell types
The authors compare RNA expression profiles across three human cell types following infection with MERS-CoV
Read More...Innovative Treatment for Reducing Senescence and Revitalizing Aging Cells through Gene Silencing
Cellular senescence plays a key role in aging cells and is attributed to a number of disease and pathology. These authors find that genetic editing of both RPS6KB1 and PPARGC1A revitalizes a human skin fibroblast cell line.
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