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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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Application of gene therapy for reversing T-cell dysfunction in cancer

Hyun Lee et al. | Aug 25, 2022

Application of gene therapy for reversing T-cell dysfunction in cancer

Since cancer cells inhibit T-cell activity, the authors investigated a method to reverse T-cell disfunction with gene therapy, so that the T-cells would become effective once again in fighting cancer cells. They used the inhibition of proprotein convertases (PCSK1) in T cells and programmed death-ligand 1 (CD274) in cancer cells. They observed the recovery of IL-2 expression in Jurkat cells, with increased recovery noted in a co-culture sample. This study suggests a novel strategy to reactivate T cells.

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The Effects of Ultraviolet Light on Escherichia coli

Kodoth et al. | Sep 07, 2015

The Effects of Ultraviolet Light on <em>Escherichia coli</em>

In this study E. coli bacteria was exposed to small UV lights currently used in school laboratories to see the effect on colony growth. This project explores how UV radiation methods could be applied in common households to inhibit bacterial growth.

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RNAi-based Gene Therapy Targeting ZGPAT Promotes EGF-dependent Wound Healing

Lee et al. | Nov 15, 2021

RNAi-based Gene Therapy Targeting ZGPAT Promotes EGF-dependent Wound Healing

Wound-healing involves a sequence of events, such as inflammation, proliferation, and migration of different cell types like fibroblasts. Zinc Finger CCCH-type with G-Patch Domain Containing Protein (ZGPAT), encodes a protein that has its main role as a transcription repressor by binding to a specific DNA sequence. The aim of the study was to find out whether inhibiting ZGPAT will expedite the wound healing process by accelerating cell migration. This treatment strategy can provide a key to the development of wound healing strategies in medicine and cellular biology.

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Modular mimics of neuroactive alkaloids - design, synthesis, and cholinesterase inhibitory activity of rivastigmine analogs

Yu et al. | Sep 12, 2022

Modular mimics of neuroactive alkaloids - design, synthesis, and cholinesterase inhibitory activity of rivastigmine analogs

Naturally occurring neuroactive alkaloids are often studied for their potential to treat Neurological diseases. This team of students study Rivastigmine, a potent cholinesterase inhibitor that is a synthetic analog of physostigmine, which comes from the Calabar bean plant Physostigma venenosum. By comparing the effects of optimized synthetic analogs to the naturally occurring alkaloid, they determine the most favorable analog for inhibition of acetylcholinesterase (AChE), the enzyme that breaks down the neurotransmitter acetylcholine (ACh) to terminate neuronal transmission and signaling between synapses.

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Green Tea Extract as an Environmentally Friendly Antibacterial Agent Against Pseudomonas syringae pv. tomato on Plants

Lo et al. | Oct 27, 2015

Green Tea Extract as an Environmentally Friendly Antibacterial Agent Against <i>Pseudomonas syringae pv. tomato </i>on Plants

Plant pathogens can cause significant crop loss each year, but controlling them with bactericides or antibiotics can be costly and may be harmful to the environment. Green tea naturally contains polyphenols, which have been shown to have some antimicrobial properties. In this study, the authors show that green tea extract can inhibit growth of the plant pathogen Pseudomonas syringae pv. tomato and may be useful as an alternative bactericide for crops.

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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 Bioactive Ingredients in Niuli Lactucis Agrestibus Possess Anticancer Effects

Zhu et al. | Sep 17, 2019

The Bioactive Ingredients in Niuli Lactucis Agrestibus Possess Anticancer Effects

In​ the​ field​ of​ medicine,​ natural​ treatments​ are​ becoming ​increasingly ​vital ​towards ​the ​cure ​of ​cancer. Zhu et al. wanted to investigate the effects of lettuce extract on cancer cell survival and proliferation. They used an adenocarcinoma cell line, COLO320DM, to determine whether crude extract from a lettuce species called Niuli​ Lactucis Agrestibus​ would affect cancer cell survival, migration, and proliferation. They found that Niuli extract inhibited cancer cell survival, increased expression of cell cycle inhibitors p21 and p27, and inhibited migration. However, Niuli extract did not have these effects on healthy cells. This work reveals important findings about a potential new source of anti-colorectal cancer compounds.

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Detection and Control of Spoilage Fungi in Refrigerated Vegetables and Fruits

Chari et al. | May 16, 2021

Detection and Control of Spoilage Fungi in Refrigerated Vegetables and Fruits

Food spoilage leads to a significant loss in agricultural produce each year. Here, the authors investigate whether certain essential oils can protect against fungus-mediated spoilage of fruits and vegetables. Their results suggest that the compounds they tested might indeed inhibit fungal growth, at various temperatures, a promising result that could reduce food wasting.

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