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We first set out to
2021-09-24
We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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GPR agonistic activity was evaluated for the human
2021-09-24
GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin
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By regulation of synaptic glutamate concentration glutamate
2021-09-24
By regulation of synaptic glutamate concentration, glutamate transporters play an important role in limiting glutamate signaling and controlling the activation of glutamate receptors (Rimmele and Rosenberg, 2016). Reduced glutamate transport is thought to underlie the pathogenesis of numerous neurol
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A number of experimental data declare a tight
2021-09-24
A number of experimental data declare a tight interdependence between the pathological changes of glutamate transport in LB Agar Miller and consequent alterations in glutamate transport and activity/expression of glutamate metabolizing enzymes in platelets (Aliprandi et al., 2005, Behari and Shriva
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br WM astrocytes Grey matter astrocytes express
2021-09-24
WM astrocytes Grey matter astrocytes express a variety of GluR types that have both physiological and pathophysiological significance [87]. Non-NMDA GluR are also expressed in WM astrocytes [40], although the functionality of these receptors has not been tested. The fibrous astrocytes that popula
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A breakthrough in the understanding of the
2021-09-24
A breakthrough in the understanding of the unique properties of GPX4-downregulation-induced cell death was accomplished when Seiler et al. in 2008 demonstrated the role of 12/15-lipoxygenase (12/15-LOX), a polyunsaturated fatty angiotensin receptor blockers metabolizing enzyme [92], in the execution
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br Materials and methods br Results br Discussion Since
2021-09-24
Materials and methods Results Discussion Since early times, herbs and their extracted substances have been used as foods and medicinal resources worldwide (Petrovska, 2012). A Ginger is one of the most important and oldest spices, consisting of the prepared and sun-dried rhizomes of Zingibe
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In vitro studies have described the kinetic parameters of th
2021-09-24
In vitro studies have described the kinetic parameters of the KDM4A catalytic site (cKDM4A) (Figure 1C) (23); the kcat/KM (kcat as the catalytic constant and KM as the Michaelis constant) values represent how fast the enzyme reacts with the substrate once it encounters the substrate, where the value
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Introduction Hepatocellular carcinoma HCC is the fifth most
2021-09-23
Introduction Hepatocellular carcinoma (HCC) is the fifth most lethal malignant tumor worldwide and is the second leading cause of cancer-related death [1]. For HCC patients, Sulindac virus (HBV) infection is the important causative risk factor in Asia-Pacific regions [[2], [3], [4]]. In China, mor
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br Conclusion br Disclosure of interest br Acknowledgement
2021-09-23
Conclusion Disclosure of interest Acknowledgement Introduction Vitamin B6 has long been recognized as a cofactor for many enzymes, especially those involved in amino pterostilbene metabolism. Apart from its role as coenzyme, recent studies are unveiling a new role of vitamin B6 as a che
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br Future perspectives sGC signaling is important in the mai
2021-09-23
Future perspectives sGC signaling is important in the maintenance of multiple physiological functions. sGC is localized to cell membranes with both sGC Cys modifications and heme regulation identified as the crucial components in regulating sGC activity. Specifically, S-nitrosation of several com
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Given the involvement of dysregulated S nitrosylation in
2021-09-23
Given the involvement of dysregulated S-nitrosylation in multiple pathological conditions, a number of approaches to regulate S-nitrosylation therapeutically are being tried in multiple indications [18]. In the lung, GSNO releasing compounds and GSNOR inhibitors are being considered as potential the
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We also examined possible involvement of the NF B
2021-09-23
We also examined possible involvement of the NF-κB signaling pathway in GSK-3 inhibitor-induced suppression of PGE2 production, whereas GSK-3 inhibitors did not have a significant effect on IκB phosphorylation/degradation or NF-κB nuclear translocation. These results are consistent with a previous p
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BIX 01294 mg Molecular modeling studies also revealed insign
2021-09-23
Molecular modeling studies also revealed insignificant differences in ligand-receptor interaction energies between R and S enantiomers of LPCs or their 2-OMe-analogues, suggesting that enantiomers of a particular structure should exert similar GPR119-mediated biological effect. Indeed, when studied
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During pain signal transmission glutamate is released into
2021-09-23
During pain signal transmission, glutamate is released into the synaptic cleft, which, in turn, causes activation of N-methyl-d-aspartate (NMDA) receptors and hence neurotransmission across the synapse occurs. The synaptic concentration and resultant activity of glutamate are controlled by excitator
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