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To enhance the impact of
2021-12-21

To enhance the impact of GD2 as an immune target in this cancer, we investigated a novel strategy to upregulate expression on the cell surface of EwS cells by an epigenetic agent, based on the following rationale. Biosynthesis of GD2 and other gangliosides during organ development is driven by stage
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On the other hand G a GLP could
2021-12-21

On the other hand, G9a/GLP could also alter neuronal function without directly altering the transcription level of particular plasticity-related protein: the consolidation of early-LTP to late-LTP, as well as the reversal of mGluR-LTD by G9a/GLP inhibition required PKMζ translation and its downstrea
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The more important effect of pitolisant is
2021-12-21

The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced caspofungin sale release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcoleptic teen
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Metallothioneins MTs that are intracellular proteins respons
2021-12-21

Metallothioneins (MTs) that are intracellular proteins responsible for the maintenance of metal homeostasis are involved in arsenic toxicity (Kita et al., 2006). Four major MT isoforms have been reported so far, MT1, MT2A, MT3 and MT4. The synthesis of MT1 and MT2A isoforms in mammal cells can be in
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The number of small molecule GSK inhibitors
2021-12-21

The number of small molecule GSK-3 inhibitors is continuously rising and many have been tested in animals. These studies have provided additional support for specific roles of GSK-3 in neuronal functions under both normal and pathological conditions. Inhibition of GSK-3 has profound effect on neurop
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In the present study we observed a decrease in body
2021-12-21

In the present study, we observed a decrease in body weight gain in Tg rats. It is uncertain whether this effect is due to Denr, Gpr81, or Gpr109a. In this regard, Gpr81 mice have been reported to have reduced body weight gain [28]. Moreover, a small clinical study has reported that obese patients
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Here we show that lactate
2021-12-21

Here we show that lactate activates the Gi-coupled receptor GPR81, which is exclusively expressed on adipocytes, and that lactate released from adipocytes in response to glucose and insulin mediates insulin-induced antilipolysis by activation of GPR81. Results Discussion Nutrients and their m
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Interestingly zaprinast administration not only prevents the
2021-12-21

Interestingly, zaprinast administration not only prevents the development of hypersensitivity but also enhances opioid effectiveness. Opioids have long been considered among the most effective drugs used to treat pain (Watkins et al., 2005; Mika et al., 2013; Szczudlik et al., 2014a, Szczudlik et al
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dapagliflozin Although domain organization had been clearly
2021-12-21

Although domain organization had been clearly delineated by the 4.3-Å structure of T4-γ-secretase [], atomic modeling of the side chains had to wait for the 3.4-Å structure []. In total, 598 residues in the transmembrane region and 632 residues in the ECD were modeled for the four components of huma
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The mechanisms underlying the inhibitory
2021-12-21

The mechanisms underlying the inhibitory effects of n-3 FAs on neoplasia have not been completely elucidated. Until recently, the emphasis has been on the ability of n-3 FAs to compete for the pathways that lead to the synthesis of pro-inflammatory eicosanoids from arachidonic acid, an n-6 FA, there
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FPR ligands comprise structurally very diverse classes of co
2021-12-21

FPR ligands comprise structurally very diverse RGFP966 of compounds, ranging from naturally occurring peptides/proteins or “danger signals” such as PAMPs and DAMPs (see 1.1), respectively, to endogenous lipids and even various synthetic non-peptides, such as benzimidazoles, pyrazolones, pyridazine-
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FFAs are essential nutritional molecules that can also modul
2021-12-21

FFAs are essential nutritional molecules that can also modulate numerous cellular functions. Fatty ati stock quote derivatives like prostaglandins, leukotrienes lysophosphatidic acid, spinhgosine-1-phosphate and others are well documented to carry out signal transduction via G-protein coupled recep
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The Ala to Leu substitution would reduce the
2021-12-21

The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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The site of paracetamol action remains
2021-12-21

The site of paracetamol action remains controversial. Some publications are in favor of a central action (Barrière et al., 2013, Dogrul et al., 2012, Mallet et al., 2010, Pickering et al., 2006), while others report a peripheral action (Dani et al., 2007, Ferreira et al., 1978). FAAH is a ubiquitous
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P Benzoxaborole substituted macrocyclic compounds based on
2021-12-20

P4-Benzoxaborole-substituted macrocyclic compounds based on ITMN-191 scaffold were prepared using a general scheme as shown in . ITMN-191 was prepared by following a patent procedure. The P4 BOC group was removed by treatment with TFA in dichloromethane to give amine . The coupling of the amine to 6
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