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Trifluoromethyl ketones and fluorophosphates were the first
2022-06-18

Trifluoromethyl ketones and fluorophosphates were the first generation FAAH inhibitors identified. They showed good in vitro FAAH inhibition potency, but most of them exhibited poor selectivity for FAAH over other serine hydrolases (such as the triacylglycerol hydrolase and the membrane-associated h
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To enhance the impact of GD as an immune target
2022-06-18

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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br Experimental br Acknowledgments We thank Mintek and Rhode
2022-06-18

Experimental Acknowledgments We thank Mintek and Rhodes University for generous financial support and permission to publish these findings. T.O.O. gratefully acknowledges Obafemi Awolowo University, Ile-Ife, Nigeria for study leave. Introduction There are ∼35.3 million people living with
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In the CNS histamine is
2022-06-18

In the CNS, alpha adrenergic blockers is known to regulate sleep and wakefulness, learning and memory, feeding, and energy. Here, we address its actions in relation to CNS disorders, and emphasize potential clinical applications of histamine receptor ligands (Table 1). In addition, as the effect of
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Introduction Histamine Imidazolyl ethylamine is an important
2022-06-18

Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric TPCA-1 secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, among others. Histamine exerts it
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Experimental conditions may be critical to explain one model
2022-06-18

Experimental conditions may be critical to explain one model or the other. The matter of Hippo-driven cytoplasmic sequestration (Varelas et al., 2008) of active SMAD complexes (Varelas et al., 2008) vs. TßR basolateral relocalization upon epithelial polarization (Nallet-Staub et al., 2015) as mechan
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In addition to narrowing a wide knowledge gap in
2022-06-18

In addition to narrowing a wide knowledge gap in Hh developmental biology research, improved understanding of Disp structure and function is likely to also be relevant to cancer. A growing body of evidence supports that Shh facilitates tumor–stroma communication in a range of cancers to influence tu
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Distribution of Iodine labeled ANP I ANP radioactivity
2022-06-18

Distribution of 125Iodine-labeled-ANP (125I-ANP) radioactivity on the cell surface, in the intracellular compartments, and in culture medium established a dynamic equilibrium of receptor-mediated 125I-ANP uptake, degradation, and release outside of Fmoc-Leu-OH (Fig. 2). A major proportion of intern
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A nitric oxide donor glyceryl trinitrite and
2022-06-18

A nitric oxide donor, glyceryl-trinitrite, and the substrate for nitric oxide, l-arginine, have been used to treat preterm labor. However, these studies are preliminary. The beneficial effect of nitric oxide donors needs to be confirmed by more controlled studies. The probable pitfall of using nitri
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Interestingly studies from Sahai and
2022-06-18

Interestingly, studies from Sahai and colleagues in cancer-associated fibroblasts have revealed that YAP is required for the acquirement of a stiff ECM in the tumor microenvironment (Calvo et al., 2013). Subsequently, this stiffening of the matrix can activate YAP, thus creating a feed-forward loop.
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Resolving the molecular details of glyco proteome variation
2022-06-17

Resolving the molecular details of (glyco)proteome variation in different tissues and organs of the human body is critical for the understanding of human biology and disease [59]. Glycoproteomic analysis of disease-related tissues and cells has provided valuable information to identify promising tar
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Finally the formation of a regular
2022-06-17

Finally, the formation of a regular network of fusion glycoproteins in their post-fusion state is not exclusive of vesiculovirus G. More or less regular networks have been also observed with other class III fusion glycoproteins such as pseudorabies gB [85] and several class II fusion glycoproteins [
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To further investigate if GPR was the functional target of
2022-06-17

To further investigate if GPR40 was the functional target of these phenylpropiolic PR-171 australia analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK29
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br Materials animals and methods
2022-06-17

Materials, animals and methods Results Discussion This study presents mice with a missense point mutation in R258 of FFAR1 that has functional consequences. Firstly, in islets of Ffar1R258W/R258W mice, both the physiological agonist palmitate and the synthetic agonist TUG-469 were unable to
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Here we reported series of carbohydrate modified compounds
2022-06-17

Here, we reported series of carbohydrate-modified compounds containing a dibromo substituted benzene ring which was derived from the red alga (). The conformation flexibility of nucleoside transporters and their polyol structures give them many unique biological properties as we have described ear
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