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Emerging evidence has shown that pharmacological FXR agonism
2022-05-19

Emerging evidence has shown that pharmacological FXR agonism attenuates chronic alcohol treatment-induced liver injury and steatosis [18], [19], while whole-body FXR knockout worsens alcohol-induced liver injury [19]. This suggests that FXR plays an important role in ALD development. However, defici
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Thus our data demonstrate that
2022-05-18

Thus, our data demonstrate that polymorphisms of GSTP1-1 differentially mediate activation of Prdx6 peroxidase activity, providing a platform to imply that contingent upon their GSTP genotype, individuals will have significant differences in mounting an antioxidant response, particularly affecting p
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Our synthetic approach to GPR antagonists was designed so th
2022-05-18

Our synthetic approach to GPR55 antagonists was designed so that many different structures could be accessed to rapidly explore initial SAR, along with validating or modifying our current model (). The synthesis begins with the coupling of a carboxylic sphingosine receptor to 4-piperidone by first
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As disclosed in our preceding
2022-05-18

As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, PHA-665752 sale lacks
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br Materials and methods br Results br
2022-05-18

Materials and methods Results Discussion and conclusions Our data demonstrate that native and 2-OMe-LPC analogues are GPR119 ligands and activate insulin secretion from βTC-3 pancreatic cells. LPC 18:1 was the first proposed endogenous ligand for GPR119 [1], however natural LPC has limited
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With an ever increasing incidence rate of
2022-05-18

With an ever-increasing incidence rate of type 2 diabetes and obesity, it is imperative to develop new therapeutic regimes that may provide a benefit both in terms of efficacy and tolerability. The existing portfolio of drugs for the treatment of metabolic disorders, primarily type 2 diabetes and ob
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We were able to obtain
2022-05-18

We were able to obtain several crystalline forms of CHAV Gth. The first one corresponded to the post-fusion conformation [14]. The comparison of this structure with that of VSV-Gth post-fusion conformation revealed that the PHD is the most divergent domain, with the largest differences confined to t
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br Brief overview of the glutamate
2022-05-18

Brief overview of the glutamate system and rationale for targeting the glycine site of NMDARs In the central nervous system (CNS), glutamate is the major excitatory neurotransmitter and works in concert with gamma-aminobutyric g protein coupled receptors (GABA), the primary inhibitory neurotrans
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br Methods GLUT DS was diagnosed
2022-05-18

Methods GLUT1DS was diagnosed either when analysis of the SLC2A1 gene showed a pathogenic mutation and/or when cerebrospinal fluid (CSF) analysis met the criteria for GLUT1DS: a CSF Necrostatin 1 below the 10th percentile, a cerebrospinal fluid (CSF) to blood ratio below the 25th percentile and
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br Discussion In the present
2022-05-18

Discussion In the present study, we have demonstrated the effect of a high-fat diet upon wild-type and glut3 pregestational female phenotype and shown that it leads to obesity due to an increase in white adipose tissue contributing to the overall fat mass. Despite this observed obesity along with
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In the liver ghrelin has
2022-05-18

In the liver, ghrelin has opposite effects to insulin on the expression of the enzyme PEPCK, thereby promoting gluconeogenesis and also causing a decrease in glucose uptake and fatty Alsterpaullone australia oxidation (Rigault et al., 2007). Ghrelin also stimulates hepatic lipogenesis de novo in a
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There are multiple docking platforms suitable for
2022-05-17

There are multiple docking platforms suitable for use with nucleic W-7 hydrochloride receptors. These include: DOCK v4-6 (UCSF) [[68], [69], [70]], AutoDock (Scripps) [71], AutoDock Vina (Scripps) [72], GOLD (Cambridge Crystallographic Data Centre) [73], Surflex-DOCK (BioPharmics) [74], Glide (Schrӧ
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LXRs are physiological regulators of cholesterol and lipid m
2022-05-17

LXRs are physiological regulators of cholesterol and lipid metabolism and influence glucose metabolism. In addition, they have been shown to repress transcription of certain pro-inflammatory genes (Jakobsson et al., 2012; Ogawa et al., 2005; Terasaka et al., 2005). Thus, LXRs can either activate or
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The molecular target of N BPs is farnesyl
2022-05-17

The molecular target of N-BPs is farnesyl diphosphate synthase (FPPS), a crucial enzyme at the branch point of cholesterol and isoprenoid synthesis in the mevalonate pathway [5]. Because they bind calcium ions, N-BPs accumulate quickly in the skeleton and are internalised by osteoclasts, leading to
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According to previous methods several mobile phase compositi
2022-05-17

According to previous methods, several mobile phase compositions and gradient programmes were assayed to get the best resolved peaks for HA and MHA [12], [13], [24]. Considering the slightly structural differences of the analytes, a mobile phase consisting in two eluents of different polarity and pH
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