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GK allosteric activators validate the
2021-11-11
GK allosteric activators validate the importance of GK from a therapeutic perspective, but the nature of allosteric activation of GK remains unclear. The GK allosteric activator site, the pocket where GKAs bind, is ~20 Å remote from the active site (Fig. 1A). The allosteric site is the locus of many
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Taken together previous data suggest that ghrelin signaling
2021-11-11
Taken together, previous data suggest that ghrelin signaling is causally linked to alcohol use and may regulate alcohol seeking and consummatory behaviors [[66], [67], [68]]. As such, the ghrelin system may represent a therapeutic target for AUD. Here, we provide a narrative review of the existing l
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We have previously designed an azobenzene based molecule Raz
2021-11-11
We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u
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br Introduction In addition to glucose which is the foremost
2021-11-11
Introduction In addition to glucose, which is the foremost stimulator of insulin secretion in beta-cells, other nutrients such as free fatty acids (also called non-esterified fatty acids, NEFA) contribute to glucose-stimulated insulin secretion (GSIS). Glucose triggers the processes leading to in
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Recently results obtained by our group
2021-11-11
Recently, results obtained by our group have demonstrated that hEECs are able to secrete NPY into the extracellular medium and that this peptide can induce an increase in the [Ca]i of these cells (Jacques et al., 2003b). In light of these results and those obtained in this study, we can speculate th
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It has been demonstrated that RA regulates
2021-11-11
It has been demonstrated that RA regulates gene BYL-719 through an epigenetic mechanism during stem cell and cancer cell differentiation. In neuroblastoma cells, RA induced neural maturation through RET gene transcriptional activation by increasing H3K4me3 levels at the promoter region and demethyl
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Many studies support that the increase of P improves
2021-11-10
Many studies support that the increase of P4 improves embryonic survival and reduces embryonic losses in ruminants [6,[18], [19], [20]]. However, experimental results are variable, contradictory and often inconclusive results. Certain studies showed that administration of GnRH or hCG after artificia
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Next we investigated the accumulation
2021-11-10
Next, we investigated the accumulation of [3H]-ribavirin in fresh villous fragments of human placenta, which provide a physiologically relevant, well-described and validated model for assessing drug interactions with ENTs [32], [35], [69], [70]. The uptake of [3H]-ribavirin was time-dependent and si
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Glutamate activates cationic glutamate gated channels i
2021-11-10
Glutamate activates cationic glutamate-gated channels (i.e. ionotropic glutamate receptors) that mediate the fast excitatory actions of glutamate. It also activate G protein-coupled receptors, named metabotropic glutamate receptors (mGluRs) (Pin and Bettler, 2016). The eight subtypes of mGluRs are k
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Caffeine decreased EAAT and EAAT expression levels
2021-11-10
Caffeine decreased EAAT1 and EAAT2 Fluorescein-12-dUTP levels in P2 fraction, as well as [3H]d-aspartate uptake; however, as soon as caffeine is removed from incubation, [3H]-d-Aspartate uptake is recovered to control levels, eliminating the possibility of caffeine as a cell death inducer. In resu
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In conclusion we have designed and
2021-11-10
In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date,
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br Introduction Major depressive disorder MDD is a disease w
2021-11-10
Introduction Major depressive disorder (MDD) is a disease with poorly recognized etiology. Currently used antidepressant drugs, which mainly affect synaptic neurotransmitter levels, show full clinical efficacy in only one third of patients (Rush, 2007). Thus it is now generally accepted that the
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br Do the actions of GLP R agonists on the
2021-11-10
Do the actions of GLP-1R agonists on the vascular endothelium account for GLP-1R agonist-mediated cardioprotection? The previous section highlighted the recent clinical evidence from cardiovascular outcomes studies supporting the notion that GLP-1R agonists confer cardioprotective actions in pati
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How do myofibroblast sources compare between bone
2021-11-10
How do myofibroblast sources compare between bone marrow and other organs? Perivascular SGX-523 with MSC properties significantly contribute to fibrosis in muscle, fat, skin, heart, kidney, lung, and liver (reviewed in Iwayama et al., 2015) and activate Gli1 in many of these organs (Kramann et al.,
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Seizures in turn selectively modulate the expression of
2021-11-10
Seizures, in turn, selectively modulate the influenza a virus of GalR in the hippocampus. Thus, pilocarpine-induced SE led to a 30% downregulation of GalR2 without affecting GalR1 (personal communication with T. Bartfai, Scripps Research Institute). Therefore, despite the fact that GalR2 could have
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