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Studies utilising GPR mice however report different effects
2022-10-12
Studies utilising GPR55−/− mice, however, report different effects of GPR55 on body weight and insulin sensitivity. Genetic deletion of GPR55 appears to have no effect on overall body weight 5, 6, 7. However, one of these studies found increased fat deposition and insulin resistance in GPR55−/− mice
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In humans the effect of GnRH and
2022-10-12
In humans, the effect of GnRH and hCG on trophoblast invasion was found to be mediated through extracellular matrix remodeling by facilitating the activity of MMP2 and MMP9 [13], [18], [44]. Both LY-411575 are collagenases that degrade extracellular matrix. In canines, this has not yet been investi
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br Transporter based brain targeting
2022-10-12
Transporter-based brain-targeting nano-DDS Drug delivery to the central nervous system (CNS) is still challenging due to the bloodbrain barrier (BBB)53., 54.. The BBB is a natural defense barrier protecting the topirimate mg from harmful substances. Since only selected, neutral, lipophilic small
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Riluzole Tight junctions regulate the transfer of ions as
2022-10-12
Tight junctions regulate the transfer of ions as well as small molecules across endothelial barriers (Li et al., 2015). We also investigated whether resistin affects tight junctions, which play an important role in the conformation of polarized endothelial barriers (Matsuzaki et al., 2010). A previo
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br Acknowledgements br Introduction Aminoacyl tRNA synthetas
2022-10-12
Acknowledgements Introduction Aminoacyl-tRNA synthetases catalyze the formation of an ester bond between an amino Triciribine synthesis and the 3′ end of a tRNA in a two-step reaction. First, the amino acid is activated and an enzyme-bound adenylate intermediate is formed. Then, the amino aci
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A key limiting factor in the semi quantitative analysis
2022-10-12
A key limiting factor in the semi-quantitative analysis of changes in the nuclear-to-cytoplasmic distribution of glucokinase is the large intercellular heterogeneity of Acyclovir of glucokinase in both isolated hepatocytes in vitro and also in liver in vivo[13], [23], [24], [26], [36]. This necessi
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The MeO CFO phen yl group was then selected for
2022-10-12
The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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It is notable that pharmacological
2022-10-12
It is notable that pharmacological or genetic inhibition of GCGR signaling results in the engagement of a number of compensatory mechanisms that potentially impact glucose control. These include alpha-cell hyperplasia [2], [11], [12], [13] and increased beta-cell proliferation under low insulin cond
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Considerable evidence links sustained GCG administration to
2022-10-12
Considerable evidence links sustained GCG administration to the reduction of food intake, enhancement of energy expenditure and weight loss in rodent and human studies [16], [17], [18]. Moreover, patients presenting with GCG-producing tumors frequently manifest severe weight loss, through mechanisms
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Defining the cooperation between molecular pathways within h
2022-10-11
Defining the cooperation between molecular pathways within highly complex biological systems, such as those between immune cell networks and target tissues is certainly a hard task. Recently, there are many investigations in the pathogenesis of renal graft rejection, one of the most evident investig
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The finding of histamine action on ASICs also raises the
2022-10-10
The finding of histamine action on ASICs also raises the question about possible action of other histamine receptor ligands. In the present work we selected several compounds and performed electrophysiological testing of their action on recombinant homomeric ASIC1a and ASIC2a. Nα-methylhistamine is
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br Introduction Histamine was generally accepted as a
2022-10-10
Introduction Histamine was generally accepted as a neurotransmitter in 1984, when histamine was first identified to be located in tuberomamillary nucleus (TM) of the brain (Watanabe et al., 1984). In mammals, histaminergic neurons play an important role in regulating multiple physiological activi
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Based on our results we propose three possible mechanisms of
2022-10-10
Based on our results, we propose three possible mechanisms of HER2 loss after trastuzumab-based therapy (Fig. 3). The first possibility is a result of the differential effects of treatments on clonal subsets. In breast cancer, such selective pressure has been suggested to preferentially eradicate HE
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br Discussion By using ultra deep
2022-10-10
Discussion By using ultra-deep sequencing, we conducted a thorough assessment of HCV-NS3 protease variants in chronic PI-naïve patients infected with HCV-1a and HCV-1b under telaprevir-based triple therapy at baseline and after 4weeks of treatment. Several synonymous and non-synonymous substituti
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In summary we have designed and explored
2022-10-10
In summary, we have designed and explored synthetic routes towards novel acylsulfamoyl benzoxaborole-based HCV NS3 protease inhibitors. Interestingly, the resulting, unoptimized P1–P3 and P2–P4 macrocyclic inhibitors were equipotent in an enzyme assay and somewhat less potent in replicon assays, com
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