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High-throughput virtual screening of novel dihydropyrimidine monastrol analogs reveals robust structure-activity relationship to kinesin Eg5 binding thermodynamics

Shern et al. | Jan 20, 2021

High-throughput virtual screening of novel dihydropyrimidine monastrol analogs reveals robust structure-activity relationship to kinesin Eg5 binding thermodynamics

As cancer continues to take millions of lives worldwide, the need to create effective therapeutics for the disease persists. The kinesin Eg5 assembly motor protein is a promising target for cancer therapeutics as inhibition of this protein leads to cell cycle arrest. Monastrol, a small dihydropyrimidine-based molecule capable of inhibiting the kinesin Eg5 function, has attracted the attention of medicinal chemists with its potency, affinity, and specificity to the highly targeted loop5/α2/α3 allosteric binding pocket. In this work, we employed high-throughput virtual screening (HTVS) to identify potential small molecule Eg5 inhibitors from a designed set of novel dihydropyrimidine analogs structurally similar to monastrol.

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Estimation of cytokines in PHA-activated mononuclear cells isolated from human peripheral and cord blood

Subbiah et al. | Mar 09, 2022

Estimation of cytokines in PHA-activated mononuclear cells isolated from human peripheral and cord blood

In this study, the authors investigated the time-dependent cytokine secretion ability of phyto-hemagglutinin (PHA)-activated T cells derived from human peripheral (PB) and cord blood (CB). They hypothesized that the anti-inflammatory cytokine, IL-10, and pro-inflammatory cytokine, TNFα, levels would be higher in PHA-activated T cells obtained from PB as compared to the levels obtained from CB and would decrease over time. Upon PHA-activation, the IL-10 levels were relatively high while the TNFα levels decreased, making these findings applicable in therapeutic treatments e.g., rheumatoid arthritis, psoriasis, and organ transplantation.

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Testing the Effects of Resveratrol, Apigenin, and Glucosamine to Effectively Reduce Prostate Cancer Cell Proliferation, Migration Levels, and Increase Apoptosis

Yang et al. | Apr 16, 2020

Testing the Effects of Resveratrol, Apigenin, and Glucosamine to Effectively Reduce Prostate Cancer Cell Proliferation, Migration Levels, and Increase Apoptosis

The current five-year survival rate of metastasized prostate cancer is only 30% and occurs in every one in nine men. Researchers have shown that people with a type of dwarfism called Laron’s Syndrome are immune to cancer due to their low levels of insulin-like growth factor-1 (IGF-1). For this reason, experimentally modifying the level of IGF-1 could provide better insight into whether lowering the levels of IGF-1 in prostate cancer cell lines (e.g. PC-3) could be an effective treatment to reduce their rates of proliferation and migration and increase apoptosis. We selected three compounds, which researchers have shown decrease IGF-1 levels, to test and combine to determine which is the most promising.

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The Effect of Wind Mitigation Devices on Gabled Roofs

Kaufman et al. | Feb 20, 2021

The Effect of Wind Mitigation Devices on Gabled Roofs

The purpose of this study was to test devices installed on a gabled roof to see which reduced the actual uplift forces best. Three gabled birdhouse roofs were each modified with different mitigation devices: a rounded edge, a barrier shape, or an airfoil. The barrier edge had no significant effect on the time for the roof to blow off. The addition of airfoil devices on roofs, specifically in areas that are prone to hurricanes such as Florida, could keep roofs in place during hurricanes, thus reducing insurance bills, overall damage costs, and the loss of lives.

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The feeling of beauty in music: Relaxing and not confusing

Jain et al. | Sep 07, 2022

The feeling of beauty in music: Relaxing and not confusing

Here, the authors sought to better understand how and why people experience beauty in music. They explored this fundamental aesthetic response by considering numerous emotional responses of participants to diverse musical excerpts using a 42-item Aesthetic Emotions Scale assessment. They found that the highly nuanced emotional experience of beauty in music includes positive, negative, and knowledge-related feelings.

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Association between nonpharmacological interventions and dementia: A retrospective cohort study

Yerabandi et al. | Jan 09, 2023

Association between nonpharmacological interventions and dementia: A retrospective cohort study
Image credit: Ross Sneddon

Here, the authors investigated the role of nonpharmacological interventions in preventing or delaying cognitive impairment in individuals with and without dementia. By using a retrospective case-control study of 22 participants across two senior centers in San Diego, they found no significant differences in self-reported activities. However, they found that their results reflected activity rather than the activity itself, suggesting the need for an alternative type of study.

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Starts and Stops of Rhythmic and Discrete Movements: Modulation in the Excitability of the Corticomotor Tract During Transition to a Different Type of Movement

Lim et al. | Aug 27, 2018

Starts and Stops of Rhythmic and Discrete Movements: Modulation in the Excitability of the Corticomotor Tract During Transition to a Different Type of Movement

Control of voluntary and involuntary movements is one of the most important aspects of human neurological function, but the mechanisms of motor control are not completely understood. In this study, the authors use transcranial magnetic stimulation (TMS) to stimulate a portion of the motor cortex while subjects performed either discrete (e.g. throwing) or rhythmic (e.g. walking) movements. By recording electrical activity in the muscles during this process, the authors showed that motor evoked potentials (MEPs) measured in the muscles during TMS stimulation are larger in amplitude for discrete movements than for rhythmic movements. Interestingly, they also found that MEPs during transitions between rhythmic and discrete movements were nearly identical and larger in amplitude than those recorded during either rhythmic or discrete movements. This research provides important insights into the mechanisms of neurological control of movement and will serve as the foundation for future studies to learn more about temporal variability in neural activity during different movement types.

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Behavioral Longevity: The Impact of Smoking, Alcohol Consumption, and Obesity on Life Expectancy

Han et al. | Oct 03, 2019

Behavioral Longevity: The Impact of Smoking, Alcohol Consumption, and Obesity on Life Expectancy

In this article, the authors look into what is already known about the factor affecting longevity and determine the importance of behavioral factors including alcohol consumption, smoking, and obesity on longevity. The authors quantify data from over 150 countries and, interestingly, find that the impact each factor has on longevity is at least in part dependent on the country's economic development status. Overall, they conclude that an average person’s life expectancy can increase by more than 3 years if smoking and alcohol consumption is reduced by a half and weight is decreased by 10%.

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Comparing the Effectiveness of Popular Treatments for Swelling and Scarring

Benavides et al. | Jul 08, 2020

Comparing the Effectiveness of Popular Treatments for Swelling and Scarring

Numerous specialty treatments claim to reduce swelling and scarring; however, it is unknown if these treatments are more effective than less expensive treatments. In an attempt to determine if one outperforms the other, treatments were applied to the same subject following bilateral orthopedic foot surgery. No difference was found the specialty treatments compared to more cost-effective treatments.

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