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br Conflict of interest br Acknowledgements br Introduction
2022-06-17
Conflict of interest Acknowledgements Introduction Second generation antipsychotic drugs (SGAs) such as olanzapine are widely used in treating individuals with schizophrenia and bi-polar disorder and are increasingly prescribed for other conditions such as anxiety (Pringsheim and Gardner, 2
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Recently multiple receptor agonists have been developed to t
2022-06-17
Recently, multiple receptor agonists have been developed to treat type II diabetes (Finan et al., 2013, Finan et al., 2015). We have tested novel dual GLP-1/GIP receptor agonists that showed good neuroprotective effects that are superior to single GLP-1 analogues (Cao et al., 2016, Jalewa et al., 20
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All data were analyzed using SAS software version SAS Instit
2022-06-17
All data were analyzed using SAS software (version 9.3, SAS Institute Inc., Cary, NC). Because of very low FFAR1 protein detection (at the detection limit or no signal) in 3 H-BHB cows, quantification was not possible within a linear range and therefore these animals were omitted from the statistica
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To understand the impact of
2022-06-17
To understand the impact of alterations in az628 synthesis zinc homeostasis, the role of Zn2+ as a neurotransmitter has to be appreciated. Certain regions of the brain including the neocortex and hippocampus harbour so-called “zincergic” (or “gluzinergic”) neurons, where Zn2+ is co-released with gl
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The receptor binding assay used in
2022-06-17
The receptor binding assay used in our previous study demonstrated that propofol competitively binds to FPR1, thus blocking the downstream signal transduction of FPR1 and inhibiting neutrophil immune activities [8]. In this study, we assessed the pharmacological action of fMMYALF in the presence of
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br Introduction GPR also known as free fatty
2022-06-17
Introduction GPR40 (also known as free fatty Eplerenone mg receptor 1), a member of the G-protein coupled receptor (GPCR) family, is expressed in pancreatic beta cells, intestine and the central nervous system (Bekinschtein et al., 2008; Itoh et al., 2003). It is activated by medium- and long-ch
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br Experimental procedures br Results
2022-06-17
Experimental procedures Results Discussion The data herein confirm the well documented neuroinflammatory effect of TLR3 activation following systemic administration of the viral mimetic poly I:C and the associated acute sickness response which includes fever, reduced body weight and allodyn
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br Drugs approved or in development To
2022-06-16
Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis
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br Methods br Results br Discussion Exercise
2022-06-16
Methods Results Discussion Exercise results in a remarkable redistribution of blood flow, which increases in active skeletal muscles but decreases in the splanchnic circulation. The regional blood flow in the kidney, spleen, stomach and intestine was measured by using the microsphere techni
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Among the isoforms of heme oxygenases HO HO and HO
2022-06-16
Among the 3 isoforms of heme oxygenases (HO-1, HO-2, and HO-3), HO-1 expression is inducible, and it catalyzes the degradation of heme to biliverdin, carbon monoxide (CO) and free Fe. The Fe is then stored in ferritin, limiting its ability to participate as a catalyst through the Fenton reaction and
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br Mechanism of HH pathway activation in NSCLC Despite
2022-06-16
Mechanism of HH pathway activation in NSCLC Despite the role of the HH pathway in basal cell carcinoma and medulloblastoma, it has been postulated that epithelial tumors do not demonstrate cell autonomous HH ligand activity. The main evidence comes from the study by Yauch et al showing no correla
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Another interesting approach is to use partial
2022-06-16
Another interesting approach is to use partial agonists as starting point to develop specific antagonists like done in earlier decades [64], [65]. Possible indications for an attenuation of the NO/sGC signalling pathway might be specific neuronal disorders: an involvement in the aetiology of migrain
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We show that pharmacological inactivation
2022-06-16
We show that pharmacological inactivation of GSTP1 over a sustained period does not show any observable toxicity, and not only prevents breast tumor growth but even slows established breast tumor growth in mice. A highly potent GSTP1 inhibitor, ezatiostat (developed by Telik Inc.) has passed phase
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The absolute requirement for substrate prephosphorylation ra
2022-06-16
The absolute requirement for substrate prephosphorylation raised the possibility that short phosphorylated peptides might serve as selective substrate competitive inhibitors. A set of phosphorylated peptides patterned after known GSK-3 substrates was generated and shown to inhibit GSK-3 in vitro in
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To characterize the binding receptor for HIV
2022-06-16
To characterize the binding receptor for HIV-1 gp120 in autophagy, we used the CXCR4 inhibitor AMD3100 and NMDA receptor inhibitor MK801 along with gp120 to treat the cardiomyocytes. Our data demonstrated that inhibition of the NMDA receptor significantly blocked the increase of gp120 induced autoph
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