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Optimization of the tetrahydroindazole series led to the dis
2022-04-15

Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ()
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G quadruplex structures can be resolved by helicases Consist
2022-04-15

G-quadruplex structures can be resolved by helicases. Consistently, many helicases are aberrantly expressed in cancer Flutamide [47]. In this study, we correlated HOXC10 expression with that of all helicases using a microarray dataset derived from 759 breast cancer patients [36] and discovered that
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The effect of GC on Fgf was not directly
2022-04-15

The effect of GC on Fgf21 was not directly dependent on ileal Fgf15 because basal Fgf21 gsk-3 was similar in Fgf15+/+ and Fgf15−/− mice. Moreover, GC treatment induced similar Fgf21 up-regulation in both strains. Fxr activation has been reported to increase Fgf21 expression and secretion [28]. In m
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FFAs are essential nutritional molecules that can also
2022-04-15

FFAs are essential nutritional molecules that can also modulate numerous cellular functions. Fatty ARRY-380 receptor derivatives like prostaglandins, leukotrienes lysophosphatidic acid, spinhgosine-1-phosphate and others are well documented to carry out signal transduction via G-protein coupled rece
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br To explore further the functional impact of
2022-04-15

To explore further the functional impact of the similarity of the UTY and KDM6A proteins, the FANTOM5 human dataset was analysed to determine whether or not the genes were expressed at the same time in the same tissues (which would suggest that they are controlled by the same regulators) or with o
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The more important effect of pitolisant is related
2022-04-15

The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced Lin28 1632 release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcoleptic teenagers
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Another important outcome of reducing hypothalamic HIF in DI
2022-04-15

Another important outcome of reducing hypothalamic HIF in DIO was the increase in gliosis and hypothalamic inflammation. Both experimental and human studies have shown that hypothalamic inflammation plays an important role in obesity by inducing resistance to anorexigenic signals, such as insulin an
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Carteolol HCl mg A more quantitative view of kinase specific
2022-04-14

A more quantitative view of kinase specificity suggests a continuum of phosphorylation rates for the various substrates of a particular kinase (Figure 4A). Such differences in ‘substrate quality’ can arise from variations in phosphorylation site or docking sequences and may explain why the timing or
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In contrast to RhoA Rac and Rap which are stimulated
2022-04-14

In contrast to RhoA, Rac1 and Rap1 which are stimulated by platelet activators and inhibited by NO/PKG, the GTPase ADP-ribosylation factor 6 (Arf6) is regulated in the reverse way. Platelet agonists like thrombin, collagen, or ADP, reduce Arf6-GTP levels, whereas NO and PGI2 oppose this reduction [1
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One previously unreported discovery is
2022-04-14

One previously unreported discovery is that Ptgds is alternatively spliced, such that partial removal of exon 3 correlates with higher levels of regeneration. The absence of exon 3 likely affects the functionality of the final product. The structure of Ptgds is that of the typical lipocalin β-barrel
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GPR A a G protein coupled receptor located mainly
2022-04-14

GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic UNC1999 synthesis [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-
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SecinH3 receptor Abnormal expression and higher activity of
2022-04-14

Abnormal expression and higher activity of GLO I have been detected more in various tumor SecinH3 receptor than in normal cell samples., , , , , , , Among cancer cell lines, lung carcinoma cells frequently showed higher GLO1 activity. Human NSCLC cell line NCI-H522 cells possess high activity and ex
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In agreement with the results obtained from GluR
2022-04-14

In agreement with the results obtained from GluR-A−/− mice, mice in which the NR1 subunit of the NMDA receptor has been selectively deleted from the CA3 subfield of the hippocampus displayed normal acquisition of the standard reference memory version of the watermaze task (Nakazawa et al., 2002), bu
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In the GLUT family glucose transporter GLUT is
2022-04-14

In the GLUT family, glucose transporter 1(GLUT1) is primarily responsible for basal glucose uptake and maintenance of glucose basal metabolism in cells (Olson and Pessin, 1996). High GLUT1 expression occurred in various types of human cancers, like brain tumor, lung cancer and esophageal cancer (Nis
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Next the effects of a
2022-04-14

Next, the effects of a phenyl group at the 3- and 4-positions of the furan on GCGR affinity were investigated (). Surprisingly, despite the lack of a 4-phenyl group at the furan, compound exhibited almost the same GCGR affinity as compound . On the other hand, when the phenyl group at the 3-positio
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