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br Materials and methods br Results br Discussion
2021-09-23
Materials and methods Results Discussion In this study, we demonstrated that zaprinast (a cGMP-PDE inhibitor) induced the intracellular calcium mobilization in the Lidocaine coexpressing GPR35 and Gqi5, Gqo5, or Gα16. Induction of intracellular calcium mobilization by zaprinast in the GPR3
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The atherosclerosis development requires additional pro infl
2021-09-23
The atherosclerosis development requires additional pro-inflammatory response in the vascular tissue, promoting increased levels of adhesion molecules such as VCAM-1 (vascular cell adhesion molecule-1) and ICAM-1 (intercellular adhesion molecule-1). Cytokines such as TNF-α and IL-1β are able to upre
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In summary through medicinal chemistry design and computer a
2021-09-23
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on d
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GPR is a member of the G protein coupled
2021-09-23
GPR119 is a member of the G protein-coupled receptor family, and is highly expressed in pancreatic β-cells and intestinal endocrine cells. It has been proposed that GPR119 agonists modulate glucose homeostasis by indirectly stimulating glucose-dependent insulin release through enhancing pancreatic c
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Neurotransmitter transporters are rapidly recycled from and
2021-09-23
Neurotransmitter transporters are rapidly recycled from and to the membrane. For instance, the GABA transporter GAT1 is recycled in a calcium and depolarization dependent manner. GAT1 located in the plasma membrane is internalized to a subpopulation of small vesicles different from the classical neu
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br Computational details and modeling All calculations were
2021-09-23
Computational details and modeling All calculations were performed using the density functional B3LYP [34] method, implemented in Gaussian03 program [35]. The structures of reactants, transition states, intermediates, and products were optimized using the 6-31+G(d) basis set for the H, C, N, O an
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br Experimental procedure br Acknowledgments This research
2021-09-23
Experimental procedure Acknowledgments This research was supported by funds provided by NIH/NIAAA grant P01 AA020683 and the Waggoner Center for Alcohol and Addiction Research. Introduction Acute mesenteric ischemia (AMI) is still associated with a high mortality rate, and currently, an ea
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Introduction Carbohydrates are some of the most stereochemic
2021-09-23
Introduction Carbohydrates are some of the most stereochemically complex biological molecules found in nature. In addition to their energetic and structural roles in living systems, their role when covalently linked to proteins is critically important in a myriad of molecular recognition processes.
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br Acknowledgements br Introduction Obesity is a growing pan
2021-09-23
Acknowledgements Introduction Obesity is a growing pandemic, which becomes a global public health problem. The evidence has been readily available and mounting, demonstrating that obesity increases incidences of chronic comorbidities, such as non-alcoholic fatty liver diseases, diabetes, cardi
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br Glucocorticoid receptor and metabolic syndrome
2021-09-23
Glucocorticoid receptor and metabolic syndrome GCs acting through the GR regulate key enzymes of glucose metabolism in the liver, skeletal muscle, adipose tissue and the pancreas. In the liver, GCs regulate the expression of major gluconeogenic enzymes such as phosphoenolpyruvate carboxykinase, g
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br Materials Aspergillus oryzae GS U mg solid was
2021-09-23
Materials Aspergillus oryzae βGS (8.4 U mg−1 solid) was obtained from Sigma-Aldrich Chemicals Co. (USA). o-Nitrophenyl β-d-galactopyranoside (ONPG), sodium carbonate, zinc chloride, manganese chloride, calcium chloride and potassium chloride were procured from Sisco Research Laboratories (SRL), M
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Developmental studies have reported that some subunits of GA
2021-09-23
Developmental studies have reported that some subunits of GABAA receptors like α2 and α3 are predominantly expressed during in-utero development, and then substituted for α1 around birth in the rat hippocampus (Brooks-Kayal et al., 2001; Fritschy et al., 1994; Golshani et al., 1997; Kapur and Macdon
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We focus here on the historical discoveries that
2021-09-22
We focus here on the historical discoveries that led to the development of the concept of ferroptosis. Ferroptosis is defined as an iron-dependent form of regulated cell death, which occurs through the lethal accumulation of lipid-based reactive oxygen species (ROS) when glutathione (GSH)-dependent
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br Interference in coagulation assays Conversely to heparin
2021-09-22
Interference in coagulation assays Conversely to heparin, or heparin like Z-Ligustilide synthesis (LMWH, Fondaparinux, Sodium Danaparoid), which are catalytic inhibitors requiring the presence of AT for their activity, as depicted on Fig. 2, DiXaIs are directly targeted to Factor Xa, and are rev
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The other possibility for the
2021-09-22
The other possibility for the lack of effects of H1 receptor agonists, e.g. histamine, on the NMDAR-mediated responses is that other neurotransmitters may cause more profound effects than histamine on the gliotransmitter release from astrocytes. For example, recent studies showed that noradrenaline,
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