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br Ketone body metabolism and neuronal excitability One of t
2021-11-26
Ketone body metabolism and neuronal excitability One of the best examples of the close connection between metabolism and neuronal excitability is illustrated by the effect of ketone bodies on epileptic seizures. One third of patients suffering from epileptic seizures do not respond to conventiona
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Since KYNA concentrations are increased by aerobic
2021-11-26
Since KYNA concentrations are increased by aerobic exercise training, we have investigated if it plays a role in peripheral tissue metabolism. Here we show that KYNA regulates adipose tissue energy homeostasis through activation of Gpr35. Activation of this network stimulates the expression of lipid
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In this study we describe the role of a
2021-11-26
In this study, we describe the role of a specific species of LPI in the secretion of GLP-1 from enteroendocrine L-cells and primary cell preparations. We further demonstrate the specific role of GPR119 in LPI-dependent GLP-1 secretion. To achieve this, we downregulated GPR119 and GPR55 protein expre
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Recently a G protein coupled receptor GPR a
2021-11-26
Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of
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PRX-08066 Antibiotic treatment suggests that cancer promotin
2021-11-26
Antibiotic treatment suggests that cancer-promoting bacteria arise from the PRX-08066 of Grp109a mice. How does the lack of Gpr109a signaling lead to expansion of potentially cancer-promoting bacteria? Is this phenomenon related to improper development of intestinal Treg cells? Biome with cancer-pro
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br The presence of an
2021-11-25
The presence of an active glyoxalase pathway in an apicomplexan parasite was first reported in Plasmodium falciparum-infected erythrocytes (Vander Jagt et al., 1990). Some years later, glyoxalase I and both glyoxalase II enzymes were characterized in this parasite (Akoachere et al., 2005, Iozef et
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Pediatric cancers are fundamentally different from adult tum
2021-11-25
Pediatric cancers are fundamentally different from adult tumors and usually display a lower mutational burden and a faster growth rate. About 30% of all childhood malignancies are solid tumors and, in a majority of cases, respond well to chemotherapy. However, in particular in neuroblastoma the succ
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In conclusion we demonstrated that the atypical high
2021-11-25
In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 Hexamethonium Bromide results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This network act
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Tail group SAR of the imidazole derived analogs is
2021-11-25
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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br Conclusion In summary a series of novel GPR agonists
2021-11-25
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic WYE-132 mg motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing potent
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This study was approved by our institutional ethics committe
2021-11-25
This study was approved by our institutional ethics committee, and informed consent was obtained from each participant or legal guardian. We performed whole-genome SNP genotyping in the one unaffected and two affected siblings by using the Illumina Human 610 Genotyping BeadChip panel, which interrog
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In this study we demonstrate that the
2021-11-25
In this study, we demonstrate that the ETS transcription factor ETV5 is involved in the regulation of ghrelin system in response to the altered nutritional state. In the recent multiple GWAS studies, three single nucleotide polymorphisms (SNPs) of ETV5, rs7647305 (Thorleifsson et al., 2009; Willer e
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The effects of GHS R a blockade on alcohol related
2021-11-25
The effects of GHS-R1a blockade on alcohol-related outcomes have been examined in numerous preclinical experiments, utilizing various GHS-R1a antagonists (JMV 2959, [D-Lys3]-GHRP-6, BIM 28163) and rodent species (prairie vole, mouse, rat). In spite of methodological differences, the results consiste
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Glucocorticoid is a major regulator of body s response
2021-11-25
Glucocorticoid is a major regulator of body's response to stress (Armario, 2006). Repeated injections of the glucocorticoid corticosterone (CORT) in mice have been shown to produce an animal model of depression (Zhao et al., 2008). Further study of this phenomenon suggested that prolonged CORT expos
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br Results br Discussion Glucose homeostasis is
2021-11-25
Results Discussion Glucose homeostasis is regulated by a complex and intricate signaling network involving multiple organs. The BA nuclear receptor FXR is integrated into this regulatory network and participates in glucose handling and metabolism. Intestinal FXR favors glucose carboxypeptidase
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