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Taken together our results show that at
2022-08-17
Taken together, our results show that, at least in the in vitro cell line model, methylation within the proximal promoter region of GHSR is an important determinant of its expression; however, to determine whether this represents a physiologically and or pathophysiologically relevant event, further
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Among sensitizers tested in the previous study six
2022-08-16
Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter
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During the course of our
2022-08-16
During the course of our optimization of the diarylsulfonamide chemotype as FFA4 agonists, we identified xanthene as a potent and selective antagonist of FFA4 (). Xanthene was able to block the agonist induced intracellular Ca response elicited by both linoleic PD173955 sale and compound in comp
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As a part of our continuing
2022-08-16
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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difluprednate On the contrary the benzhydrol
2022-08-16
On the contrary, the benzhydrol series showed modest activity with EC of two digit micromole. The bulkiness of the difluprednate tail may be the reason for the low activity. Interestingly, introduction of H-bonding groups, such as OMe in and CF in , slightly improved the activity compared to the uns
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br Acknowledgments We apologize to the researchers who
2022-08-16
Acknowledgments We apologize to the researchers who were not referenced due to space limitations. We thank Dave Primm (Department of Surgery, University of Texas Southwestern Medical Center) for his critical reading of the manuscript. This work was supported by grants from the US National Institu
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Microglia after activation can show prominently
2022-08-16
Microglia after activation can show prominently pro-inflammatory but also anti-inflammatory characteristics [46]. Although the ageing process is not a pathological process, many of the age-associated changes resemble those observed under pathological conditions. An increase number of pro-inflammator
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Recently several groups reported that four orphan receptors
2022-08-15
Recently, several groups reported that four orphan receptors, GPR40, GPR41, GPR43, and GPR120, can be activated by free fatty acids. Short-chain fatty acids are specific agonists for GPR41 and GPR43 . Medium and long-chain fatty acids can activate GPR40 and GPR120 . Our previous report showed that a
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In normal tissues the expression patterns of GPR and
2022-08-15
In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet annexin v synthesis and intestinal tract [7], [20]. It is considered that the distribution of
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br Conclusion and future directions
2022-08-13
Conclusion and future directions GS is an important therapeutic target for the treatment of Alzheimer's disease. Its structure and function have been studied during the last years to understand the substrate cleavage mechanism to modulate the Aβ42 peptide production. The recent elucidation of GS
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There are many kinds of neurological disorders and
2022-08-13
There are many kinds of neurological disorders and neuropsychiatric diseases, like stroke, dementia, schizophrenia and so on. Among these disorders, the most important reason for choosing depression in our study is that FXR has already been demonstrated to regulate the function of CREB, which is clo
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br Site of expression FASTK is
2022-08-13
Site of expression FASTK is expressed in various parts of human body including heart, skeletal muscle, brain, placenta, lung, liver, kidney pancreas (Ota et al., 2004) and many other organs (Fig. 1). It has been reported that FASTK is highly expressed in pancreatic tumors, where it is involved in
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Upon LPS stimulation ERK and STAT signaling pathways were ac
2022-08-13
Upon LPS stimulation, ERK and STAT3 signaling pathways were activated in a time-dependent manner, and the phosphorylation of Y705 occurred later than that of S727 (Supplementary Fig. S5B). STAT3 is known to be phosphorylated on serine 727 (S727) by the mitogen-activated protein (MAP) kinase pathway
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Studies with GSNOR knockout mice reported decreased
2022-08-12
Studies with GSNOR knockout mice reported decreased CD4+ Pergolide mesylate receptor and increased CD19+ cells (B-cell) in the blood [31] as well as demyelination, neurodegeneration, and neuropathic pain [29]. To understand the basis of these differences in immune function of GSNOR knockout mice an
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The expression of COX has been correlated with
2022-08-12
The expression of COX-2 has been correlated with the density of amyloid plaque [65]. A study reported that IMX was effective in suppressing the expression of iNOS and IL-6, but not COX-2, in LPS-stimulated BV2 microglial cells [52]. In this study, IMX did not alter upregulation of COX-2 induced by H
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