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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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Pressure and temperature influence the efficacy of metal-organic frameworks for carbon capture and conversion

Lin et al. | May 07, 2023

Pressure and temperature influence the efficacy of metal-organic frameworks for carbon capture and conversion

Metal-organic frameworks (MOFs) are promising new nanomaterials for use in the fight against climate change that can efficiently capture and convert CO2 to other useful carbon products. This research used computational models to determine the reaction conditions under which MOFs can more efficiently capture and convert CO2. In a cost-efficient manner, this analysis tested the hypothesis that pressure and temperature affect the efficacy of carbon capture and conversion, and contribute to understanding the optimal conditions for MOF performance to improve the use of MOFs for controlling greenhouse CO2 emissions.

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Transfer Learning for Small and Different Datasets: Fine-Tuning A Pre-Trained Model Affects Performance

Gupta et al. | Oct 18, 2020

Transfer Learning for Small and Different Datasets: Fine-Tuning A Pre-Trained Model Affects Performance

In this study, the authors seek to improve a machine learning algorithm used for image classification: identifying male and female images. In addition to fine-tuning the classification model, they investigate how accuracy is affected by their changes (an important task when developing and updating algorithms). To determine accuracy, a set of images is used to train the model and then a separate set of images is used for validation. They found that the validation accuracy was close to the training accuracy. This study contributes to the expanding areas of machine learning and its applications to image identification.

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Effect of pH on the antibacterial properties of turmeric

Ganga et al. | Aug 31, 2023

Effect of pH on the antibacterial properties of turmeric

Some spices have antimicrobial or antibacterial properties that people have already tested. Turmeric has a wide variety of uses and has even been implemented in alternative medicine as a treatment for cancer, inflammation, osteoarthritis, and other diseases. We tested the antimicrobial effects of turmeric under two different pHs to characterize this effect in vitro. Decreasing the pH of a solution of turmeric may increase antibacterial properties.

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The Effect of the Stomatal Index on the Net Rate of Photosynthesis in the Leaves of Spinacia oleracea, Vinca minor, Rhododendron spp, Epipremnum aureum, and Hedera spp

Segev et al. | Nov 15, 2015

The Effect of the Stomatal Index on the Net Rate of Photosynthesis in the Leaves of <i>Spinacia oleracea</i>, <i>Vinca minor</i>, <i>Rhododendron spp</i>, <i>Epipremnum aureum</i>, and <i>Hedera spp</i>

The density of stomata, or stomatal index, in plant leaves is correlated with the plant's rate of photosynthesis, and affected by the plant's climate. In this paper, authors measure the stomatal index of five plant species to derive their rates of photosynthesis. These results could help track changes in plants' photosynthetic rates with changing climate.

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Fluorescein or Green Fluorescent Protein: Is It Possible to Create a Sensor for Dehydration?

Joshi et al. | Dec 09, 2019

Fluorescein or Green Fluorescent Protein: Is It Possible to Create a Sensor for Dehydration?

Currently there is no early dehydration detection system using temperature and pH as indicators. A sensor could alert the wearer and others of low hydration levels, which would normally be difficult to catch prior to more serious complications resulting from dehydration. In this study, a protein fluorophore, green fluorescent protein (GFP), and a chemical fluorophore, fluorescein, were tested for a change in fluorescence in response to increased temperature or decreased pH. Reversing the pH change did not restore GFP fluorescence, but that of fluorescein was re-established. This finding suggests that fluorescein could be used as a reusable sensor for a dehydration-related pH change.

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Effect of environment factors on the expression of soluble PDE8A1 in E. coli

Jiang et al. | Oct 25, 2022

Effect of environment factors on the expression of soluble PDE8A1 in <em>E. coli</em>

PDE8, a type of phosphodiesterase (PDE), is proven to be crucial in various cellular activities and physiological activities by influencing second messenger systems. It is involved in a wide range of diseases, including Alzheimer’s disease and various heart diseases. However, there is limited information about PDE8 selective inhibitors. This work aimed to improve the solubility and yield of PDE8 in the supernatant by exploring suitable culture conditions, including temperatures and different additives.

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Assessing CDK5 as a Nanomotor for Chemotactic Drug Delivery

Jiang et al. | Sep 08, 2022

Assessing CDK5 as a Nanomotor for Chemotactic Drug Delivery

Enzyme chemotaxis is a thermodynamic phenomenon in which enzymes move along a substrate concentration gradient towards regions with higher substrate concentrations and can be used to steer nanovehicles towards targets along natural substrate concentrations. In patients with Alzheimer’s disease, a gradient of tau protein forms in the bloodstream. Tau protein is a substrate of the enzyme CDK5, which catalyzes the phosphorylation of tau protein and can travel using chemotaxis along tau protein gradients to increasing concentrations of tau and amyloid-beta proteins. The authors hypothesized that CDK5 would be able to overcome these barriers of Brownian motion and developed a quantitative model using Michaelis-Menten kinetics to define the necessary parameters to confirm and characterize CDK5’s chemotactic behavior to establish its utility in drug delivery and other applications.

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Statistically Analyzing the Effect of Various Factors on the Absorbency of Paper Towels

Tao et al. | Dec 04, 2020

Statistically Analyzing the Effect of Various Factors on the Absorbency of Paper Towels

In this study, the authors investigate just how effectively paper towels can absorb different types of liquid and whether changing the properties of the towel (such as folding it) affects absorbance. Using variables of either different liquid types or the folded state of the paper towels, they used thorough approaches to make some important and very useful conclusions about optimal ways to use paper towels. This has important implications as we as a society continue to use more and more paper towels.

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