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Consistent with these observations impaired transduction of
2022-04-16

Consistent with these observations, impaired transduction of the glutamate signal by NMDARs (i.e., NMDA receptor hypofunction [NRH]) by parvalbumin-containing GABAergic inhibitory interneurons is implicated in mediating social deficits, a domain of psychopathology responsible for poor functional out
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Next we designed substituents of
2022-04-16

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 MUTYH associated polyposis br MUTYH and its metal
2022-04-16

MUTYH-associated polyposis MUTYH and its metal cofactors MUTYH harbors two vital cofactors, both of which are located remotely from the active site (Fig. 6). One of these cofactors, a [4Fe-4S]2+(Fe-S) cluster, is chelated by four Cys residues in the N-terminal domain, and positions an Fe-S clu
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Always some extra effort may
2022-04-16

Always, some extra effort may make great progress in sensing platform, for example, Ma's group discovered luminescent iridium (Ⅲ) complexes which were highly selective for G-quadruplex DNA and Al3+, then they utilized these complexes to develop a series of G-quadruplex-based probes and chemosensor r
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Ethanol decreased the value of desensitization for GluR Di C
2022-04-15

Ethanol decreased the τ-value of desensitization for GluR-Di. Coexpression of stargazin or γ4 further increased the effect of ethanol on desensitization (Fig. 3A, B). The highest ethanol concentration tested (200mM) reduced the τ-value by 16.5±4.9% (n=5) in the control receptors and by 29.3±9.3% (n=
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In the present study compared to diabetic control
2022-04-15

In the present study, compared to diabetic control rats, hepatic glucose-6-phosphatase activity was significantly decreased in both SE and METF treated diabetic animals, with the latter producing greater reduction in glucose-6-phosphatase activity. This observation is consistent with the claim of Ta
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GLP and glucose dependent insulinotropic
2022-04-15

GLP-1 and glucose-dependent insulinotropic peptide (GIP) are gut hormones secreted from intestinal L CNQX and K cells, respectively. Together, these hormones account for the vast majority of the incretin effect, the enhanced postprandial insulin secretion observed in healthy adults (Dupre et al., 1
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Initially we carried out gap
2022-04-15

Initially, we carried out gap-FRAP experiments using the two-photon configuration of the confocal microscope. A SR101-positive astrocyte was targeted and a 5 × 5 μm square area was exposed to a laser illumination (5 flashes of 5 s each during 25 s). This procedure resulted in a bleaching of this ast
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Our own search towards aryl imidazole derived GSMs led to
2022-04-15

Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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br Materials and methods br Results
2022-04-15

Materials and methods Results Discussion Zn2+ is an extremely abundant transition metal in the synaptic vesicles of hippocampal glutamatergic mossy fibers and remains a key factor in the modulation of neuronal plasticity (Assaf and Chung, 1984). Disruption of Zn2+ homeostasis is associated
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The chemical structure of BAs consists
2022-04-15

The chemical structure of BAs consists of a steroid nucleus with an acidic side chain. They are amphipatic molecules characterized by a hydrophilic α-face and a hydrophobic β-face. The hydrophobic pocket of the FXR LBD interacts with BAs largely through the β-face. The α-face contains several hydrox
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Bile acids BAs are critical for facilitating the absorption
2022-04-15

Bile acids (BAs) are critical for facilitating the histone methyltransferase of dietary lipids and lipid-soluble vitamins in the intestines [6], [7]. At physiological levels, BAs function as signaling molecules and activate specific nuclear receptors [farnesoid X receptor (FXR), pregnane X receptor
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SYR-322 Endothelial cells receive a variety of information
2022-04-15

Endothelial cells receive a variety of information from the environment which finally guides them through all phases of neovascularization. Angiogenic signals enhance the proliferation of endothelial cells, upregulated resistance to apoptosis, alterations within proteolytic balance, reorganization o
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Several small molecules such as erastin and RSL
2022-04-15

Several small molecules, such as erastin and RSL3, are reported to induce ferroptosis in both normal and cancer Erastin [21,22]. We confirmed that erastin-induced growth inhibition is an ideal ferroptosis model for cardiomyocytes. The erastin inhibits the growth of H9c2 cells in a Fe-dependent mann
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Computational approaches such as docking and classical molec
2022-04-15

Computational approaches such as docking and classical molecular dynamics (MD) are now commonly used to study the structure and dynamics of proteins as well as associated protein-ligand interactions [12]. A fundamental requirement of MD in order to accurately determine the behavior of a protein over
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