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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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Trajectories Between Cigarette Smoking and Electronic Nicotine Delivery System Use Among Adults in the U.S.

Primack et al. | Apr 30, 2020

Trajectories Between Cigarette Smoking and Electronic Nicotine Delivery System Use Among Adults in the U.S.

In this study, the authors characterized the trends of cigarette use amongst people who do and don't use electronic nicotine delivery systems (or ENDS). This was done to help determine if the use of ENDS is aiding in helping smokers quit, as the data on this has been controversial. They found that use of ENDS among people either with or without previous cigarette usage were more likely to continue using cigarettes in the future. This is important information contributing to our understanding of ways to effectively (and not effectively) reduce cigarette use.

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Combating drug resistance in cancer cells: Cooperative effect of green tea and turmeric with chemotherapeutic drug

Nair et al. | Jul 27, 2020

Combating drug resistance in cancer cells: Cooperative effect of green tea and turmeric with chemotherapeutic drug

The major drawback of chemotherapy regimens for treating cancer is that the cancerous cells acquire drug resistance and become impervious to further dose escalation. Keeping in mind the studied success of herbal formulations with regard to alternative treatments for cancer, we hypothesized that the use of a chemotherapeutic drug and proprietary herbal formulation, HF1, would combat this phenomenon when administered with common chemotherapeutic drug 5FU. Results demonstrated a cooperative effect between HF1 and 5FU on the drug resistant cell line, implying that administration of HF1 with 5FU results in cell death as measured by MTT assay.

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Phospholipase A2 increases the sensitivity of doxorubicin induced cell death in 3D breast cancer cell models

Lee et al. | Mar 30, 2022

Phospholipase A2 increases the sensitivity of doxorubicin induced cell death in 3D breast cancer cell models

Inefficient penetration of cancer drugs into the interior of the three-dimensional (3D) tumor tissue limits drugs' delivery. The authors hypothesized that the addition of phospholipase A2 (PLA2) would increase the permeability of the drug doxorubicin for efficient drug penetration. They found that 1 mM PLA2 had the highest permeability. Increased efficiency in drug delivery would allow lower concentrations of drugs to be used, minimizing damage to normal cells.

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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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Association of agenesis of the corpus callosum with epilepsy and anticonvulsant drug treatment

Steger et al. | Feb 21, 2023

Association of agenesis of the corpus callosum with epilepsy and anticonvulsant drug treatment
Image credit: Robina Weermeijer on Unsplash

Agenesis of the Corpus Callosum (ACC) is a birth defect where an infant’s corpus callosum, the structure linking the brain’s two hemispheres to allow interhemispheric communication, fails to develop in a typical manner during pregnancy. Existing research on the connection between ACC and epilepsy leaves significant gaps, due to the lack of focused investigation. One important gap is the degree to which ACC may impact the course of epilepsy treatment and outcomes. The present study was conducted to test the hypotheses that epilepsy is highly prevalent among individuals with ACC, and that those with both ACC and epilepsy have a lower response rate to anticonvulsant drugs than other patients treated with anticonvulsant drugs. A weighted average of epilepsy rates was calculated from a review of existing literature, which supported the hypothesis that epilepsy was more common among individuals with ACC (25.11%) than in the general population (1.2%). An empirical survey administered to 57 subjects or parents of subjects showed that rate of intractable epilepsy among study subjects with both ACC and epilepsy was substantially higher than the rate found in the general population, indicating that individuals with both conditions had a lower response rate to the anticonvulsant drugs. This study contributes novel results regarding the potential for concurrence of ACC and epilepsy to interfere with anticonvulsant drug treatment. We also discuss implications for how medical professionals may use the findings of this study to add depth to their treatment decisions.

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Fitness social media is positively associated with the use of performance-enhancing drugs among young men

Tamaki et al. | Feb 01, 2024

Fitness social media is positively associated with the use of performance-enhancing drugs among young men
Image credit: Samuel Girven

Here the authors investigated the relationship between fitness-related social media and the high usage of performance-enhancing drugs (PEDs) specifically by men in the US age 18-35. In a survey with 149 participants they identified that young men that use fitness-related social media are more likely to use PEDs. Their results suggest the necessity to consider potential risk behaviors which may be related to social media consumption.

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