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In addition to the increase of extracellular glutamate ICH
2021-09-08

In addition to the increase of extracellular glutamate, ICH can also increase the levels of reactive oxygen species (ROS) and oxidative stress. Although the products of red blood cell lysis and plasma components, as well as the excitotoxic effect of glutamate have been to increase oxidative damage (
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br Funding sources This work was
2021-09-08

Funding sources This work was supported, in part, by NIH GM115388 to BGM. Acknowledgements Introduction Glucokinase (GCK) plays a central role in the regulation of glucose metabolism. Its activity is restricted to Piperlongumine with important roles in whole-body glucose homeostasis [1].
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Previous attempts to minimize the contribution of the compen
2021-09-08

Previous attempts to minimize the contribution of the compensatory changes due to chronic loss of Gcgr, have used temporally-controlled reduction of glucagon levels by alpha-cell ablation, glucagon immunoneutralization, and the use of small molecule or antibody glucagon receptor antagonists [10], [3
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To identify inhibitors of the Hh
2021-09-08

To identify inhibitors of the Hh/GLI signaling pathway from natural resources, we have recently reported the successful construction of a cell-based screening assay system for the Hh/GLI signaling pathway (Fig. 1). This is an assay using a GLI-dependent luciferase reporter in human keratinocyte cell
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A relatively independent review of the history of
2021-09-08

A relatively independent review of the history of the discovery of GABA (and L-glutamate) as neurotransmitters in the CNS can be found in ‘When and why amino acids?’ in the in 2010 by Kresimir Krnjevic , who spent a post-doc in Canberra in 1956–1958. Introduction The insect RDL GABA receptor is
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Through the analysis of various synthetic
2021-09-08

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Cathepsin K Activity Fluorometric Assay Kit motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in
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The investigation in vitro revealed that aldolase as well as
2021-09-08

The investigation in vitro revealed that aldolase, as well as FBPase, has affinity to α-actinin, one of the structural protein of the Z-line (Rakus et al., 2003a, Mamczur et al., 2005). Therefore, the existence of in vivo heterologous complex, consisting of aldolase, FBPase and α-actinin has been po
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The initial beta carboline derivatives used in the in silico
2021-09-07

The initial beta-carboline derivatives used in the in silico docking experiments were prepared using the procedure outlined in . Harmol, , was -alkylated with -Boc-protected alkylamines in the presence of cesium carbonate to give and . The carbamate protecting group was removed under acidic conditio
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Analysis of the thermosensory responses conferred by chimeri
2021-09-07

Analysis of the thermosensory responses conferred by chimeric proteins suggests that both the ECD and ICD of AFD-rGCs contribute to their thermoresponsive properties. The presence of the GCY-18 or GCY-23 ICD and TMD in chimeric protein combinations generally corresponds to a higher or lower , respec
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Given the involvement of dysregulated S nitrosylation in mul
2021-09-07

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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To assess the roles of GPR and GPR
2021-09-07

To assess the roles of GPR120 and GPR40 in malignant properties of pancreatic cancer cells, we generated GPR120 and GPR40 knockdown (PANC-sh120 and PANC-sh40, respectively) ML-291 mg from PANC-1 (Fig. 2A). While no difference of cell growth rate between control PANC-RFP cells and PANC-sh120 cells wa
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ceramide The inhibition of NSAIDs towards GLOI provides a
2021-09-07

The inhibition of NSAIDs towards GLOI provides a direction for the development of novel effective GLOI inhibitors. Although the inhibitory activity of indomethacin was determined and the interactions between it ceramide and GLOI were probed by NMR titration experiments, no detailed inhibitory mechan
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In summary activated A AR exacerbated
2021-09-07

In summary, activated A2AR exacerbated the reverse transport function of endothelial EAATs through a direct or indirect pathway depending on PKA and glutamate levels in response to OGD in vitro, but A2AR inhibition quickly restored the normal transport function. Moreover, the key mechanisms by which
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In this study we investigated the contribution of GCK
2021-09-07

In this study, we investigated the contribution of GCK, G6PC, and PCK expression to glycemia in diabetes. We examined liver tissue from 40 obese subjects: 12 had normal glucose tolerance (NGT) and 28 had type 2 diabetes. Materials and methods Results Discussion This study aimed to investig
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LbGlcK crystallized as a ligandless dimer in the asymmetric
2021-09-07

LbGlcK crystallized as a ligandless dimer in the asymmetric unit of space group P21 (Fig. 1a) with two identical subunits stabilized by a large contact surface area of 2295 Å2 (13% of the total surface area) as determined by the Protein Interfaces, Surfaces, and Assemblies (PISA) server [18]. Each m
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