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In our study the changes in
2022-03-07

In our study, the changes in the α4 and δ subunit expression were accompanied by a significant increase in γ2 subunit expression in almost all analysed hippocampal structures in the fully kindled animals. In contrast, an acute injection of PTZ at a convulsive dose (55mg/kg) evoked a potent decrease
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The effect of GC on Fgf was not directly dependent
2022-03-07

The effect of GC on Fgf21 was not directly dependent on ileal Fgf15 because basal Fgf21 dihydroquercetin 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
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TXNIP interacts with various proteins including
2022-03-07

TXNIP interacts with various proteins, including NLRP3 (Yoshihara et al., 2014, Zhou et al., 2010). Emerging evidence suggests that TXNIP plays a role in ER stress-mediated cell death and in the NLRP3 inflammasome activation step (Abderrazak et al., 2015, Lerner et al., 2012, Oslowski et al., 2012,
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br Introduction Farnesoid X receptor
2022-03-07

Introduction Farnesoid X receptor (FXR) is a bile salicin regulated nuclear receptor highly expressed in the liver, intestine, kidney and adrenal glands in rodents.1, 2, 3, 4 FXR regulates transport proteins, the bile salt export pump (BSEP) and the organic solute transporter α (OSTα) that are in
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Binding of FGFs to FGFRs leads to
2022-03-07

Binding of FGFs to FGFRs leads to receptor dimerization, resulting in the transphosphorylation of a tyrosine in the activation loop of the kinase domain. Subsequently, the activated FGFRs phosphorylate their intracellular receptor substrates, particularly FGFR substrate 2 (FRS2) and phospholipase Cγ
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br RESULTS br DISCUSSION In this study
2022-03-07

RESULTS DISCUSSION In this study, we found impaired apoptosis in the peripheral blood of RA patients when compared with peripheral blood from normal controls. Our previous studies have shown that the number of CD4 + T 5720 increased while regulatory T (Treg) cells diminished in the peripheral
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Penciclovir Data are expressed as means SE Statistical signi
2022-03-07

Data are expressed as means±SE. Statistical significance was determined by the Student's -test or ANOVA with post hoc Bonferroni test. A value of Penciclovir expressing human FPPS. Western blot analysis showed a clear band, which indicated the overexpression of FPPS, in U87MG cells (A, insert). Expo
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Evidence demonstrating the interplay between hypoxia and the
2022-03-07

Evidence demonstrating the interplay between hypoxia and the dynamics of histone methylation is mounting [15], [43]. For example, hypoxia leads to an increase in H3K4me3 by inhibiting their responsible demethylase [44]. Hypoxia also leads to an increase in H3K9me2 by upregulating the methyltransfera
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Distribution of histamine receptors in the
2022-03-07

Distribution of histamine receptors in the intestines varies among species, but our findings are similar to those previously reported in humans and guinea pigs (Thurmond, 2010, Thurmond, 2015). H1 receptors were located mainly in the gastric mucosa, smooth muscle, and lymphoid tissue, corresponding
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The stability and function of the HIF protein
2022-03-07

The stability and function of the HIF-1α protein are affected by many post-translational modifications (PTMs), including hydroxylation, acetylation, ubiquitination and SUMOylation [[29], [30], [31]]. It has been shown that HIF-1α stability is regulated by LSD1 [25]; in particular, the Set9 histone m
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Compared with the tetrazole derivative
2022-03-07

Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, suc
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Numerous stimuli lead to inactivation of GSK including Growt
2022-03-07

Numerous stimuli lead to inactivation of GSK-3, including Growth Factors such as EGF (Epidermal Growth Factor), PDGF (Platelet-Derived Growth Factor), BDNF (Brain-derived neurotrophic factor), IGF (Insulin-like growth factor) and insulin (Beaulieu et al., 2009, Chen and Russo-Neustadt, 2005, Cohen a
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Calcium mobilization FLIPR assay CHO K
2022-03-07

Calcium mobilization (FLIPR) assay: CHO-K1 cells expressing an NFAT-β-lactamase reporter and the promiscuous Gα-subunit Gqi5 were stably transfected with either empty vector (pCDNA3.1, Invitrogen) or vector expressing HA-GPR81, GPR109A or GPR109B. Cells were seeded at 10,000cells/well in 384-well cu
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Also the decrease in adipocyte cAMP levels seen after an
2022-03-07

Also, the decrease in adipocyte cAMP levels seen after an acute glucose challenge in wild-type mice was strongly reduced in mice lacking GPR81, indicating that the activation of PDE3B alone was not sufficient to mediate the effect of insulin on cAMP levels and lipolytic activity. The fact that insul
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AL 8810 br Synthetic Antagonists for FFA To
2022-03-07

Synthetic Antagonists for FFA4 To date, only compounds from a single chemical series have been reported as FFA4 ‘antagonists’ (Table 1). ‘Compound 39’ (4-methyl-N-9H-xanthen-9-yl-benzenesulfonamide), now available from commercial vendors as AH-7614, was initially reported as an antagonist at this
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