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The inhibition of NSAIDs towards GLOI provides a direction
2022-06-29
The inhibition of NSAIDs towards GLOI provides a direction for the development of novel effective GLOI inhibitors. Although the inhibitory activity of indomethacin was determined and the interactions between it 1115 and GLOI were probed by NMR titration experiments, no detailed inhibitory mechanism
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Oxidative stress results from the disequilibrium between lev
2022-06-29
Oxidative stress results from the disequilibrium between levels of prooxidant molecules produced and the ability of a biological system to detoxify and neutralize the reactive molecules [14]. OS is a chronic, self-perpetuating state of damage to cells and increased inflammation resulting from the co
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Here we performed TEM and
2022-06-29
Here, we performed TEM and AFM imaging to study APE1–DNA interactions. The results showed that APE1 can dynamically polymerize on DNA in an apparently sequence-independent manner. We propose that this protein polymerization allows for scanning of the structural properties of DNA with short residence
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In the spinal cord EAAT constitutes of all
2022-06-29
In the spinal cord, EAAT1 constitutes 40% of all high-affinity EAATs, and it is abundantly present in lumbar dorsal horn (Queen et al., 2007). In physiological conditions, EAATs remove glutamate from the synaptic cleft by co-transporting glutamate and sodium into adjacent glial cells. The inefficien
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Here we used a designer receptors activated exclusively by
2022-06-29
Here, we used a designer receptors activated exclusively by designer drugs (DREADD)-based chemogenetic approach in a novel Ghsr-IRES-Cre knock-in mouse line to test whether the activity of MBH GHSR neurons is required for the normal rebound food intake following fasting. We also used the Ghsr-IRES-
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In terms of stimulation oxytocin dopamine noradrenaline
2022-06-29
In terms of stimulation, oxytocin, dopamine, noradrenaline, adrenaline and glucagon have all been reported to increase ghrelin secretion (Mundinger et al., 2006, Iwakura et al., 2011, de la Cour et al., 2007, Gagnon and Anini, 2013). Stimulatory effects on ghrelin secretion have also been observed w
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In order to facilitate the preparation of aminothiazoles con
2022-06-29
In order to facilitate the preparation of 2-aminothiazoles containing novel D-ring substitutions, a convergent synthetic route was selected which requires the synthesis of common precursor . Straightforward aromatic substitution of 3,4-difluoroacetophenone using 4-methylimidazole provided access to
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D appears to be important for
2022-06-29
D83 appears to be important for receptor function as a mutation to an alanine produced a non-functional channel. Interestingly, maintaining the charge as in D83E produced only a small reduction in GABA sensitivity. Other mutations at this position which included residues capable of hydrogen bonding
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C prevents the glutamate and erastin induced ROS accumulatio
2022-06-29
C16 prevents the glutamate- and erastin-induced ROS accumulation but does not affect the decrease in GSH, indicating that prevention of ROS accumulation by C16 is not due to the restoration of GSH levels. Instead, C16 itself possessed superoxide anion scavenging activity in vitro at similar concentr
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br Introduction A great many
2022-06-29
Introduction A great many isoprenoids with varieties of structural diversity, such as steroids, carotenoids, prenyl quinones, and natural rubber, occur in nature. All of these biosynthetic precursors are constructed by the action of prenyl chain elongating enzymes [1], [2], [3], [4]. These enzyme
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Acknowledgments The authors would like to thank members of t
2022-06-28
Acknowledgments The authors would like to thank members of the Department of Discovery Synthesis (DDS) and Biocon-Bristol Myers Squibb Research Center (BBRC) for scaling up key intermediates, analytical team for analytical experiments, lead profiling group for evaluating compounds in an in vitro AD
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Introduction Protein tyrosine phosphorylation plays
2022-06-28
Introduction Protein-tyrosine phosphorylation plays key roles in a variety of intracellular signaling pathways involved in cell proliferation, differentiation, gene expression, cell adhesion, and metabolic changes [1]. While receptor-type tyrosine kinases localize to the plasma membrane, most of no
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br Introduction Lysine acetylation is
2022-06-28
Introduction Lysine acetylation is an important post-translational modification that is found on numerous cellular proteins, including both histone and non-histone proteins [1], [2]. Dynamic acetylation and deacetylation is regulated by enzymes called histone acetyltransferases (HATs) as writers
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To identify genes with significant expression differences we
2022-06-28
To identify genes with significant 2-Guanidinoethylmercaptosuccinic Acid differences, we performed differential gene expression analysis between the two individuals with TRRAP variants (combined as biological replicates) and two unaffected controls. Gene ontology (GO) enrichment analysis of these g
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Obesity is one of the worldwide concerns with
2022-06-28
Obesity is one of the worldwide concerns, with high prevalence and adverse effects on human health and life expectancy. According to the World Health Organization (WHO), obesity is defined as abnormal or excessive fat accumulation in the body with body mass index (BMI) of 30 or more. Obesity increas
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