• Acute in vivo experiments were performed in normoglycemic SV

  2021-12-31

  

  Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding CHIR-090 control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/kg produced a

• Up to now the research about the effect of PAs

  2021-12-31

  

  Up to now, the research about the effect of PAs on inhibiting carbohydrase activity in vitro or reducing blood sugar level in vivo was mainly reported in PAs from grape seeds, Lepisanthes alata (Malay cherry) leaves, sorghum, pomegranate, cranberry and persimmon (Banerji and Banerjee, 2016, Barrett

• Post translational modifications of the GR can alter the

  2021-12-31

  

  Post-translational modifications of the GR can alter the transcriptional effects of GR activation [31], and may provide a mechanism for the interactions between cell signaling pathways and GR-mediated transcriptional activity. Dex-BSA treatment reportedly increased p38 MAPK activation in CD14-positi

• GOAT belongs to the super family of

  2021-12-31

  

  GOAT belongs to the super family of membrane-bound O-acyltransferases (MBOATs). It is encoded by the gene MBOAT4 in human. The protein GOAT is highly conserved from zebrafish to human (Yanagi et al., 2018). GOAT is ubiquitously expressed with abundant expression in the stomach and intestine (Sakata

• All of the abovementioned effects of

  2021-12-30

  

  All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra

• The improved glucose tolerance of Ffar

  2021-12-30

  

  The improved glucose tolerance of Ffar1R258W/R258W mice on HFD was unexpected. In combination with similar fasting blood glucose levels, the significant lower fasting plasma insulin of mutant mice compared to wild-type mice is indicative of improved insulin sensitivity. However, peripheral insulin r

• In terms of outcome measures statistically significant diffe

  2021-12-30

  

  In terms of outcome measures, statistically significant differences were only observed in need for invasive mechanical ventilation (23% vs 46%, p-value 0.005) and in-hospital mortality (13% vs 37%, p-value 0.002). Both these outcomes were still statistically significant following adjustment for conf

• Three additional Type I CDK and CDK kinase inhibitors have

  2021-12-30

  

  Three additional Type I CDK8 and CDK19 kinase inhibitors have also been recently reported. Orally available 3-benzylindazole 12 was discovered by optimization of compounds with HSP90 affinity to yield potent and selective CDK8 inhibitors. Compound 12 showed strong binding activity for CDK8 with an I

• P corneus is a freshwater hermaphroditic gastropod that

  2021-12-30

  

  P. corneus is a freshwater hermaphroditic gastropod that is distributed all over the world (Jopp, 2006). In previous works of our laboratory, we have characterized the activities of B-esterases and we have also reported that the exposure for 48h to chlorpyrifos inhibits ChE and CES of whole dilution

• To further investigate the possible interaction

  2021-12-30

  

  To further investigate the possible interaction of L1 with β1-sGC, a protein-ligand docking experiment was performed. Calculations were carried out with the program GOLD (version 5.2) [18], [34] and performed with the chemPLP scoring function [19], [34]. The ten lowest energy solutions presented a r

• For some agonists these stable GPR responses

  2021-12-30

  

  For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer

• br Materials and methods br Results and discussion We recent

  2021-12-30

  

  Materials and methods Results and discussion We recently found that the GlyT1 N-terminal and C-terminal sequences could be modified by phophorylation, or partially lost under pathological conditions by calcium-dependent proteolysis (Baliova and Jursky, 2005, Baliova and Jursky, 2010). While re

• br Conclusion Until recently astrocytes were recognized sole

  2021-12-30

  

  Conclusion Until recently, astrocytes were recognized solely for their maintenance role in the regulation of KW 2449 homeostasis. Nowadays, this idea has changed, it is clear that these cells play a crucial role in the regulation of neuronal activity and signal transmission. In particular, glial

• The effect of GCK NES mutations on

  2021-12-30

  

  The effect of GCK-NES mutations on enzyme kinetics and protein stability might account for the hyperglycaemia that characterizes MODY2 patients, since reduced GCK activity would increase the threshold for glucose stimulated insulin release in beta-cells [31,37,49]. However, a more in depth functiona

• br Results br Discussion Our cardiomyocyte specific GR knock

  2021-12-30

  

  Results Discussion Our cardiomyocyte-specific GR knockout mice did not show spontaneous cardiac hypertrophy unless pressure overload was given to the heart. This finding is somewhat different from previous work of a cardiomyocyte-specific GR GSK744 mouse model using GR-floxed mice with loxP i

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