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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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Phytoplankton Plastid Proteomics: Cracking Open Diatoms to Understand Plastid Biochemistry Under Iron Limitation

Nunn et al. | Feb 10, 2017

Phytoplankton Plastid Proteomics: Cracking Open Diatoms to Understand Plastid Biochemistry Under Iron Limitation

In many areas of the world’s oceans, diatoms such as Thalassiosira pseudonana are limited in growth by the availability of iron (Fe), which is an essential nutrient for diatoms. The authors of this study examined if Fe-limitation makes a significant difference in the proteins expressed within the chloroplast, the power source for diatoms, utilizing a new plastid isolation technique specific to diatoms and completing 14 mass spectrometry experiments.

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In silico modeling of emodin’s interactions with serine/threonine kinases and chitosan derivatives

Suresh et al. | Jan 10, 2022

<i>In silico</i> modeling of emodin’s interactions with serine/threonine kinases and chitosan derivatives

Here, through protein-ligand docking, the authors investigated the effect of the interaction of emodin with serine/threonine kinases, a subclass of kinases that is overexpressed in many cancers, which is implicated in phosphorylation cascades. Through molecular dynamics theyfound that emodin forms favorable interactions with chitosan and chitosan PEG (polyethylene glycol) copolymers, which could aid in loading drugs into nanoparticles (NPs) for targeted delivery to cancerous tissue. Both polymers demonstrated reasonable entrapment efficiencies, which encourages experimental exploration of emodin through targeted drug delivery vehicles and their anticancer activity.

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Down-regulation of CD44 inhibits Wnt/β-catenin mediated cancer cell migration and invasion in gastric cancer

Baek et al. | May 10, 2021

Down-regulation of CD44 inhibits Wnt/β-catenin mediated cancer cell migration and invasion  in gastric cancer

In this study, we aimed to characterize CD44-mediated regulation of the Wnt/β-catenin signaling pathway, which promotes cancer invasion and metastasis. We hypothesized that CD44 down-regulation will inhibit gastric cancer cell migration and invasion by leading to down-regulation of Wnt/β-catenin signaling. We found that CD44 up-regulation was significantly related to poor prognosis in gastric cancer patients. We demonstrated the CD44 down-regulation decreased β-catenin protein expression level. Our results suggest that CD44 down-regulation inhibits cell migration and invasion by down-regulating β-catenin expression level.

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Racemic serine is less soluble than pure enantiomers due to stronger intermolecular hydrogen bonds

Ranka et al. | Nov 18, 2021

Racemic serine is less soluble than pure enantiomers due to stronger intermolecular hydrogen bonds

Seeking to develop a better understanding of the chemical and physical properties of amino acids that compose proteins, here the authors investigated the unusual relative insolubility of racemic mixtures of D- and L-serine compared to the solubility of pure D- or L-serine. The authors used a combination of microscopy and temperature measurements alongside previous X-ray diffraction studies to conclude that racemic DL-serine crystals consist of comparatively stronger hydrogen bond interactions compared to crystals of pure enantiomers. These stronger interactions were found to result in the unique release of heat during the crystallization of racemic mixtures.

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Expression of Anti-Neurodegeneration Genes in Mutant Caenorhabditis elegans Using CRISPR-Cas9 Improves Behavior Associated With Alzheimer’s Disease

Mishra et al. | Sep 14, 2019

Expression of Anti-Neurodegeneration Genes in Mutant <em>Caenorhabditis elegans</em> Using CRISPR-Cas9 Improves Behavior Associated With Alzheimer’s Disease

Alzheimer's disease is one of the leading causes of death in the United States and is characterized by neurodegeneration. Mishra et al. wanted to understand the role of two transport proteins, LRP1 and AQP4, in the neurodegeneration of Alzheimer's disease. They used a model organism for Alzheimer's disease, the nematode C. elegans, and genetic engineering to look at whether they would see a decrease in neurodegeneration if they increased the amount of these two transport proteins. They found that the best improvements were caused by increased expression of both transport proteins, with smaller improvements when just one of the proteins is overly expressed. Their work has important implications for how we understand neurodegeneration in Alzheimer's disease and what we can do to slow or prevent the progression of the disease.

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Characterization of a UPEC DegS Mutant in vitro and in vivo

Bradley et al. | Mar 16, 2015

Characterization of a UPEC <em>DegS</em> Mutant <em>in vitro</em> and <em>in vivo</em>

DegS is an integral inner membrane protein in E. coli that helps break down misfolded proteins. When it is mutated, there is a large increase in the production of outer membrane vesicles (OMVs), which are thought to play a role in pathogenesis. This study used mutant strains of uropathogenic E. coli (UPEC) to characterize the role of DegS and OMVs on UPEC virulence.

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How Ethanol Concentration Affects Catalase Catalysis of Hydrogen Peroxide

Liu et al. | Nov 15, 2021

How Ethanol Concentration Affects Catalase Catalysis of Hydrogen Peroxide

Catalase is a critical enzyme in the human body because it is capable of converting potentially dangerous hydrogen peroxide into water and oxygen. This work asks whether ethanol affects catalase activity, as alcohol consumption has been often linked to hepatitis occurring in the liver, where catalase level is especially high, and ethanol is known to be capable of denaturing proteins. Testing different concentrations of ethanol found that higher concentrations reduced the activity of catalase. This work has important implications on the negative effects of ethanol on metabolism, in which catalase plays an important role, and protein function more broadly.

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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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The Effects of Antibiotics on Nutrient Digestion

Murea et al. | Oct 06, 2017

The Effects of Antibiotics on Nutrient Digestion

One disadvantage of antibiotic therapy is the potential for unpleasant gastrointestinal side effects. Here, the authors test whether some common antibiotics directly interfere with the digestion of protein, fat, or sugars. This study provides motivation to more carefully investigate the interactions between antibiotics and gut enzymes in order to inform treatment decisions and improve patient outcomes.

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