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Mammals have three known Gli
2022-02-17
Mammals have three known Gli proteins: Gli-1, -2 and -3. Gli-1 does not undergo proteosomal degradation and hence, remains untruncated and always acts as a transcription promoter. Gli-1 is an important target gene for Gli-2. Full-length Gli-2 accumulates when Smo is activated because activated Smo p
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However a direct effect of ROS
2022-02-17
However, a direct effect of ROS on GSNOR has also been described. Inhibition of GSNOR by ROS has been demonstrated for yeast [44], Arabidopsis[36], and Baccaurea ramiflora (Burmese grape) [45] suggesting that this could be a general mechanism of crosstalk between ROS and ·No signaling. Interestingly
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br TGR Agonists br FXR TGR Dual Agonists In
2022-02-17
TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency
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Next we designed substituents of the position
2022-02-17
Next, we designed substituents of the 6-position. Edge-to-face aromatic interaction between aromatic ring of ligand and Phe162B needed to be retained because the interaction seems to be important for tight binding. 3′-Position of the 6-phenyl group of directs to a hydrophilic space where W1 exists.
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br Material and methods br Results br Discussion Neurosteroi
2022-02-17
Material and methods Results Discussion Neurosteroids capable of blocking the NMDAR channel attract a lot of attention as possible therapeutic agents for the treatment of neurodegenerative diseases. A large number of new 29 8 with different structures have been synthesized in order to crea
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We compared the age BMI and relevant laboratory variables be
2022-02-17
We compared the age, BMI and relevant laboratory variables between the two groups of risk factor multiplicity. The results are presented in Table 7 for the women and in Table 8 for the men. The individuals with an increased erythrocyte adhesiveness/aggregation can clearly be seen to be older, more o
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Increasing evidence has shown that blockade of glutamate
2022-02-17
Increasing evidence has shown that blockade of glutamate uptake leads to aberrant behavioral consequences. For example, intracerebroventricular (i.c.v) injection or microinjection of the GLT-1 inhibitor, dihydrokainic DCG IV synthesis (DHK), into the prefrontal cortex induces anhedonia [8,9]. Micro
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br Materials and Methods br Results
2022-02-17
Materials and Methods Results Discussion A model of seizure and excitotoxicity induced by neonatal MSG administration was described recently (19) in which extracellular glutamate increased after the first and second MSG administrations were observed, the greatest increase seen following the
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br Genetic rescue of GluR A
2022-02-17
Genetic rescue of GluR-A-dependent spatial working memory Spatial working memory performance in GluR-A−/− mice can be restored by the forebrain-specific [Ala92]-p16 (84-103) of GluR-A subunits labeled with green-fluorescent protein (GFP) on an otherwise GluR-A knockout background (Schmitt et al.,
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The main aim of our study was to identify whether
2022-02-17
The main aim of our study was to identify whether glucokinase and Irs2 were required for beta cell replication induced by short-term HF diet feeding. Glucokinase plays a critical role in regulating blood glucose levels by catalysing the rate-limiting biochemical reaction of glycolysis [26,27]. In pa
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The novel Ghsr IRES Cre knock in mouse line
2022-02-17
The novel Ghsr-IRES-Cre knock-in mouse line allowed us to deconstruct the involvement of MBH GHSR-expressing neurons in mediating food intake responses using chemogenetic modulation of their neuronal activity. In our studies, hM4Di DREADD virus injections to inhibit GHSR neurons targeted several nuc
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Inhibitors of the G rdos effect include the
2022-02-17
Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic
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The NVC response in the
2022-02-17
The NVC response in the diseased or aging CU CPT 4a may be altered, including changes in both the chemical mediators of NVC, ion channel behaviour, and the dynamics of the vascular system. For example, in Alzheimer’s disease the production of NO is shown to be inhibited (Lourenço et al., 2014), hyp
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However protection against kainic acid induced injury
2022-02-17
However, protection against kainic acid-induced injury was not found by Lin et al. (2003) in the rats with AAV-GAL vector-mediated galanin overexpression, even though these animals, as mentioned earlier, exhibited attenuated of seizure severity. Although the reason for the controversy between the st
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The apparent lack of effect of
2022-02-16
The apparent lack of effect of Fas deficiency on MAV-1 replication in infected mice could be due to immunoevasion by virus inhibition of Fas activation. If that were the case, Fas deficiency would likely have minimal additional effect. HAdV infection triggers Fas internalization from the cell membra
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