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Growing evidence suggests that the glycine site
2022-04-01

Growing evidence suggests that the glycine site seems to play a pivotal role in NMDAR-related function. For example, it as 481 has been demonstrated in a hippocampal slice study that the glycine site sub-serves the spatiotemporal detection of synaptic activity (Li et al., 2009). Moreover, mice with
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In contrast to short term effects long
2022-04-01

In contrast to short-term effects, long-term exposure of beta cells to FFAs impairs insulin secretion and triggers apoptosis [13]. The deleterious effects of FFAs have been linked to altered glucose/fatty Dextran sulfate sodium salt oxidation cycle [13], decreased NADPH content [14], endoplasmic re
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Ca independent release of L
2022-04-01

Ca2+-independent release of L-[14C]glutamate and [3Н]GABA that occurs via transporters working in the reverse mode also insignificantly increased in vitamin D3 deficiency despite decreased GAT-3 and EAAC-1 Dihydrotestosterone and neurotransmitter uptake efficacy Fig. 3, Fig. 6 A). However, the upwar
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Recent studies revealed that synthetic oligomeric A
2022-04-01

Recent studies revealed that synthetic oligomeric Aβ1-42 decreased GLT-1 expression and promoted mislocalization of GLT-1 from the cell surface of primary astrocytes, leading to glutamate dyshomeostasis in synapses (Abdul et al., 2009, Scimemi et al., 2013). To address the cause for reduction of ast
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br Conclusions The results of
2022-04-01

Conclusions The results of this work showed that β-glucosidase could be efficiently immobilized onto hydroxyapatite nanoparticles in a single adsorption step. The enzyme adsorption was accomplished by coordination bonds between remaining Ca2+ sites of HA and COO− of amino acids. The immobilizatio
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br Mechanisms of action Ghrelin
2022-04-01

Mechanisms of action Ghrelin is a 28-amino Benzethonium Chloride peptide hormone primarily produced in the oxyntic mucosa of stomach, but also in other gastrointestinal tissues [7] (Fig. 1). It acts as the endogenous ligand for the ghrelin receptor [GHS-R1a] and causes the release of growth hormo
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br Discussion br Author Contributions
2022-04-01

Discussion Author Contributions Alzheimer’s disease (AD) is an age-related, chronically progressive neurodegenerative disorder affecting more than 35million people worldwide and an estimated 5.5million in the US. Current marketed drugs such as acetylcholinesterase inhibitors and the NMDA ant
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Neovascularization upon IMQ treatment was observed to differ
2022-04-01

Neovascularization upon IMQ treatment was observed to different degrees in WT and GAL3-KO mice, whereas the increase in vascular endothelial growth factor mRNA levels was genotype independent. Because we observed lower levels of the cytokines IL-17A, IL-22, IL-23, and TNF-α in IMQ-treated skin of GA
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Another small compound targeting IBAT has been evaluated in
2022-04-01

Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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Interestingly we have shown that OA
2022-04-01

Interestingly, we have shown that OA required FFAR4 to induce osteoblast gene expression in MC3T3-E1 pre-osteoblasts, but not to inhibit osteoclastogenesis in RAW264.7 murine macrophages. As previously suggested, FFAR1 may mediate the effects of OA in osteoclasts. However, FFAR1 has also been shown
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This excellent tolerability is especially interesting in the
2022-04-01

This excellent tolerability is especially interesting in the light of the fact that intravenous administration of liposomal ponatinib was predicted to yield much higher plasma concentrations as compared to the orally administered free drug. In addition, liposomal drug dose in absolute numbers was te
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The typical pharmacophore for GPR agonists contains four par
2022-04-01

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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Recently the classical view of the
2022-04-01

Recently, the classical view of the compartmentalization of the plant isoprenoid metabolism has been re-evaluated, following the demonstration of the partial peroxisomal localization of the mevalonic Paclitaxel receptor (MVA) pathway, generally regarded as cytosolic. Using GFP-tagging approaches, t
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br Concluding Remarks One of the remarkable
2022-03-31

Concluding Remarks One of the remarkable features of Hippo signaling is its sensitivity to the cytoskeleton and mechanical forces. Progress has been made recently in identifying molecular mechanisms by which the cytoskeleton can influence Hippo signaling, but among the many outstanding questions
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Epigenetic drugs such as HDAC inhibitors regulate gene expre
2022-03-31

Epigenetic drugs, such as HDAC inhibitors, regulate gene expression by affecting the activity of histone or DNA modifying enzymes and their associated transcriptional response [141]. BET bromodomain protein inhibition is another epigenetic approach for blocking the Hedgehog pathway at the downstream
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