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Cellular inhibition is caused by the
2022-07-14
Cellular inhibition is caused by the hyperpolarization of the cell and is mediated by both synaptic and extrasynaptic GABAARs. Synaptic GABAARs are sensitive to high concentrations of GABA released at the synapse and mediate phasic inhibition. In contrast, extrasynaptic GABAARs mediate tonic inhibit
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The subcellular redistribution of some metabolic enzymes is
2022-07-14
The subcellular redistribution of some metabolic enzymes is dynamic and responsive to metabolic conditions. In the absence of glucose, Glucokinase (GK) is bound to its regulatory protein in the nucleus of the hepatocyte and translocates to the cytoplasm when sugar levels increase [12]. Muscle glycog
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However at variance with the well studied R form
2022-07-14
However, at variance with the well-studied R form of FBP1 which is flat, the R state of FBP2 is diametrically different, with a perpendicular orientation of the upper and lower dimers (Barciszewski et al., 2016). The cruciform-like R state of FBP2 is stabilized by a unique hydrophobic motif called ‘
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It is well known that TLR induced
2022-07-14
It is well known that TLR4-induced inflammation is associated with behavioural alterations including fever, hypolocomotion, altered appetite, anxiety and anhedonia (Dantzer, 2006, Dantzer et al., 2008). The current data demonstrate that while PF3845 potently attenuates TLR4-induced cytokines in the
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br Conclusions br Introduction Astrocytes contribute to
2022-07-13
Conclusions Introduction Astrocytes contribute to physiological TAME function on many levels. They help maintain the physiological composition of the extracellular medium by, for instance, buffering potassium and uptake of neurotransmitters. They can also provide neurons with energy substrate
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The fact that GSK recognition of its substrate involves pre
2022-07-13
The fact that GSK-3 recognition of its substrate involves pre-phosphorylation supports the rational for using synthetic phosphorylated peptides as substrate competitive inhibitors [57]. Phosphorylated peptides derived from the N-terminal pseudosubstrate sequence of GSK-3β were very weak inhibitors o
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br Materials and methods br Results br Discussion
2022-07-13
Materials and methods Results Discussion According to the literature, zaprinast is a high-affinity agonist of GPR35 (Berlinguer-Palmini et al., 2013, Divorty et al., 2015, Taniguchi et al., 2006, Zhao et al., 2010). GPR35 RP 67580 synthesis has been identified within discrete regions of th
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In normal tissues the expression patterns of GPR and
2022-07-13
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 toremifene citrate and intestinal tract [7], [20]. It is considered that the distribution of
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fgf receptor inhibitor Currently ursodeoxycholic acid UDCA i
2022-07-13
Currently, ursodeoxycholic fgf receptor inhibitor (UDCA) is the only recommended and widely used drug in the treatment of CFLD. However, the clinical efficacy of UDCA is controversial. The most recent Cochrane review only identified a small number of trials assessing the effectiveness of UDCA [92].
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To verify DNA glycosylase AP lyase
2022-07-13
To verify DNA glycosylase/AP lyase activity we have employed a simple and efficient method to investigate based on fluorescein-labeled duplex oligonucleotides read on an automated sequencer (Allgayer et al., 2013, Lopes et al., 2007, Lopes et al., 2008). This approach using purified CpMutY proteins
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To this end we evaluated novel D analogs for selectivity
2022-07-13
To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell (+)-Apogossypol australia systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (e.
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In this study we investigated
2022-07-13
In this study, we investigated the contribution of GCK, G6PC, and PCK expression to glycemia in diabetes. We examined liver tissue from 40 obese subjects: 12 had normal glucose tolerance (NGT) and 28 had type 2 diabetes. Materials and methods Results Discussion This study aimed to investig
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br Ghrelin and energy balance
2022-07-13
Ghrelin and Prote balance To characterize the physiological role of ghrelin in energy homeostasis, ghsr−/− and ghrelin−/− mice were generated [33], [36], [41], [47]. Although ghrelin regulates the amplitude of episodic GH release, ghsr−/− mice were not dwarfs, and in fact appear identical to thei
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A group of small molecule
2022-07-13
A group of small molecule with a more promising therapeutic mechanism are known as γ-secretase modulators (GSMs), which modulate the cleavage activity of γ-secretase (and likely a host of other substrates) and specifically reduce the levels of the fibrillogenic Aβ42 peptide without altering the ε-si
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br Introduction Farnesoid X receptor FXR
2022-07-12
Introduction Farnesoid X receptor (FXR) is a bile a23187 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 inv
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