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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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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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Characterizing the association between hippocampal reactive astrogliosis, anhedonia-like behaviors, and neurogenesis in a monkey model of stress and antidepressant treatment

Kim et al. | Aug 25, 2022

Characterizing the association between hippocampal reactive astrogliosis, anhedonia-like behaviors, and neurogenesis in a monkey model of stress and antidepressant treatment

This study examined the effects of stress and selective serotonin reuptake inhibitors (SSRIs) on a measure of astrocyte reactivity in nonhuman primate (NHP) models of stress. Results showed that chronic separation stress in NHPs leads to increased signs of astrogliosis in the NHP hippocampus. The findings were consistent with the hypotheses that hippocampal astrogliosis is an important mechanism in stress-induced cognitive and behavioral deficits.

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Mutation of the Catalytic Cysteine in Anopheles gambiae Transglutaminase 3 (AgTG3) Abolishes Plugin Crosslinking Activity without Disrupting Protein Folding Properties

Pham et al. | May 02, 2014

Mutation of the Catalytic Cysteine in <em>Anopheles gambiae</em> Transglutaminase 3 (AgTG3) Abolishes Plugin Crosslinking Activity without Disrupting Protein Folding Properties

Malaria is a major public health issue, especially in developing countries, and vector control is a major facet of malaria eradication efforts. Recently, sterile insect technique (SIT), or the release of sterile mosquitoes into the wild, has shown significant promise as a method of keeping vector populations under control. In this study, the authors investigate the Anopheles gambiae transglutaminase 3 protein (AgT3), which is essential to the mating of the Anopheles mosquito. They show that an active site mutation is able to abolish the activity of the AgT3 enzyme and propose it as a potential target for chemosterilant inhibitors.

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Antibacterial effectiveness of turmeric against gram-positive Staphylococcus epidermidis

Cox et al. | Jan 10, 2022

Antibacterial effectiveness of turmeric against gram-positive <i>Staphylococcus epidermidis</i>

Infections caused by antibiotic resistance are a leading issue faced by the medical field. The authors studied the antibacterial effectiveness of turmeric against gram-positive Staphylococcus epidermidis using antibiotic sensitivity disks. They infused blank antibiotic sensitivity disks with a 5% concentrated solution of turmeric and placed them on agar plates inoculated with bacteria. Overall, there was no measurable ZOI surrounding the turmeric disk so the measurements for all trials were 0 cm, suggesting that turmeric at a 5% concentration is not an effective antibacterial against S. epidermidis.

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Homology modeling of clinically-relevant rilpivirine-resistant HIV-RT variants identifies novel rilpivirine analogs with retained binding affinity against NNRTI-resistant HIV mutations

Luk et al. | Jan 24, 2022

Homology modeling of clinically-relevant rilpivirine-resistant HIV-RT variants identifies novel rilpivirine analogs with retained binding affinity against NNRTI-resistant HIV mutations

Human immunodeficiency virus (HIV), which affects tens of millions of individuals worldwide, can lead to acquired immunodeficiency syndrome (AIDS). While there is currently no cure for HIV, the development of small molecule antiretroviral agents has greatly improved the prognosis of infected individuals, especially in developed countries. Here, the authors employ homology modeling and molecular docking towards the identification of novel rilpivirine analogs that retain high binding affinity to clinically relevant rilpivirine-resistant mutations of the HIV reverse transcriptase enzyme.

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How has California’s Shelter-in-Place Order due to COVID-19 and the Resulting Reduction in Human Activity Affected Air and Water Quality?

Everitt et al. | Feb 15, 2021

How has California’s Shelter-in-Place Order due to COVID-19 and the Resulting Reduction in Human Activity Affected Air and Water Quality?

As the world struggled to grapple with the emerging COVID-19 pandemic in 2020, many countries instated policies to help minimize the spread of the virus among residents. This inadvertently led to a decrease in travel, and in some cases, industrial output, two major sources of pollutants in today's world. Here, the authors investigate whether California's shelter-in-place policy was associated with a measurable decrease in water and air pollution in that state between June and July of 2020, compared to the preceeding five years. Their findings suggest that, by some metrics, air quality improved within certain areas while water quality was relatively unchanged. Overall, these findings suggest that changing human behavior can, indeed, help reduce the level of air pollutants that compromise air quality.

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Sepia bandensis ink inhibits polymerase chain reactions

Novoselov et al. | Sep 21, 2020

<em>Sepia bandensis</em> ink inhibits polymerase chain reactions

While cephalopods play significant roles in both ecosystems and medical research, there is currently no assembled genome. In an attempt to sequence the Sepia bandensis genome, it was found that there was inhibition from the organism during DNA extraction, resulting in PCR failure. In this study, researchers tested the hypothesis that S. bandensis ink inhibits PCR. They then assessed the impact of ink on multiple methods of DNA extraction

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