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Peptidomimetics Targeting the Polo-box Domain of Polo-like Kinase 1

Jang et al. | Aug 19, 2016

Peptidomimetics Targeting the Polo-box Domain of Polo-like Kinase 1

Polo-like kinase 1 (Plk1) is a master regulator of mitosis, initiating key steps of cell cycle regulation, and its overexpression is associated with certain types of cancer. In this study, the authors carefully designed peptides that were able to bind to Plk1 at a location that is important for its proper localization and function. Future studies could further develop these peptides to selectively target Plk1 in cancer cells and induce mitotic arrest.

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Potential Multifunctional Agents for Dual Therapy of Age-Related and Associated Diseases: Alzheimer’s Disease and Type 2 Diabetes Mellitus

Kumar et al. | Nov 13, 2019

Potential Multifunctional Agents for Dual Therapy of Age-Related and Associated Diseases: Alzheimer’s Disease and Type 2 Diabetes Mellitus

Studies show an age-related link between Alzheimer’s Disease and Type 2 Diabetes Mellitus with oxidative stress a characteristic of both. Here, methanolic fractionations and extracts of four Ayurvedic plants were assessed for their protective abilities using a number of in vitro assays. Extracts inhibited oxidative stress and reduced activity of key enzymes involved in the pathogenesis of both diseases in neuroblastoma cells.

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The sweetened actualities of neural membrane proteins: A computational structural analysis

Chauhan et al. | Nov 03, 2022

The sweetened actualities of neural membrane proteins: A computational structural analysis

Here, seeking to better understand the roles of glycans in the receptors of active sites of neuronal cells, the authors used molecular dynamics simulations to to uncover the dynamic nature of N-glycans on membrane proteins. The authors suggest the study of theinteractions of these membrane poreins could provide future potential therapeutic targets to treat mental diseases.

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The characterization of quorum sensing trajectories of Vibrio fischeri using longitudinal data analytics

Abdel-Azim et al. | Dec 16, 2023

The characterization of quorum sensing trajectories of <i>Vibrio fischeri</i> using longitudinal data analytics

Quorum sensing (QS) is the process in which bacteria recognize and respond to the surrounding cell density, and it can be inhibited by certain antimicrobial substances. This study showed that illumination intensity data is insufficient for evaluating QS activity without proper statistical modeling. It concluded that modeling illumination intensity through time provides a more accurate evaluation of QS activity than conventional cross-sectional analysis.

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Decolorization of textile dyes by edible white rot fungi

Lin et al. | Apr 29, 2022

Decolorization of textile dyes by edible white rot fungi

As fast fashion explodes in popularity, the fashion industry remains one of the most prominent industries responsible for pollution. This pollution includes a lack of treatment for textile dyes that remain toxic or carcinogenic as they persist in wastewater. To resolve this, the authors of this study set out to determine the efficacy of using edible white rot fungi for cell-based biodegradation of textile dyes into harmless chemicals. This method takes advantage of fungi found in excess from the fungi industry, decreasing food waste while addressing textile waste in tandem.

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Quantitative NMR spectroscopy reveals solvent effects in the photochemical degradation of thymoquinone

Mandava et al. | Dec 16, 2023

Quantitative NMR spectroscopy reveals solvent effects in the photochemical degradation of thymoquinone

Thymoquinone is a compound of great therapeutic potential and scientific interest. However, its clinical administration and synthetic modifications are greatly limited by its instability in the presence of light. This study employed quantitative 1H nuclear magnetic resonance (NMR) spectroscopy to identify the effect of solvation on the degradation of thymoquinone under ultraviolet light (UV). It found that the rate of degradation is highly solvent dependent occurs maximally in chloroform.

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Developing anticholinergic drugs for the treatment of asthma with improved efficacy

Wong et al. | Jul 05, 2023

Developing anticholinergic drugs for the treatment of asthma with improved efficacy
Image credit: Wong et al.

Anticholinergics are used in treating asthma, a chronic inflammation of the airways. These drugs block human M1 and M2 muscarinic acetylcholine receptors, inhibiting bronchoconstriction. However, studies have reported complications of anticholinergic usage, such as exacerbated eosinophil production and worsened urinary retention. Modification of known anticholinergics using bioisosteric replacements to increase efficacy could potentially minimize these complications. The present study focuses on identifying viable analogs of anticholinergics to improve binding energy to the receptors compared to current treatment options. Glycopyrrolate (G), ipratropium (IB), and tiotropium bromide (TB) were chosen as parent drugs of interest, due to the presence of common functional groups within the molecules, specifically esters and alcohols. Docking score analysis via AutoDock Vina was used to evaluate the binding energy between drug analogs and the muscarinic acetylcholine receptors. The final results suggest that G-A3, IB-A3, and TB-A1 are the most viable analogs, as binding energy was improved when compared to the parent drug. G-A4, IB-A4, IB-A5, TB-A3, and TB-A4 are also potential candidates, although there were slight regressions in binding energy to both muscarinic receptors for these analogs. By researching the effects of bioisosteric replacements of current anticholinergics, it is evident that there is a potential to provide asthmatics with more effective treatment options.

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Analysis of complement system gene expression and outcome across the subtypes of glioma

Mudda et al. | May 17, 2023

Analysis of complement system gene expression and outcome across the subtypes of glioma
Image credit: National Cancer Institute

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.

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