• Moreover we have demonstrated that

  2021-12-23

  

  Moreover, we have demonstrated that internalization and subcellular trafficking of NPRA, using IF staining (IFS) and co-IP of plasma membrane, endosomal, lysosomal, and recycling endosome markers to follow intracellular trafficking and signaling by confocal IF microscopy (CIF) and immunoblotting (I

• imatinib mesylate In summary we have designed and optimized

  2021-12-23

  

  In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstra

• In both families GPR A mRNA

  2021-12-23

  

  In both families, GPR109A mRNA in kidney fat was positively correlated with NEFA as a tendency. A positive correlation between this fat depot and insulin was observed in lean-type cows. In fat-type cows, mesenteric GPR109A mRNA correlated positively with insulin and negatively with urea on a moderat

• br Introduction Given the growing

  2021-12-23

  

  Introduction Given the growing acceptance of ergothioneine (ET) as a biologically important agent with potential therapeutic applications [[1], [2], [3], [4]] it is increasingly important to clearly establish the role of the organic cation transporter (novel) type 1 (OCTN1). OCTN1 was discovered

• Long non coding RNAs lncRNAs are mRNA

  2021-12-23

  

  Long non-coding RNAs (lncRNAs) are mRNA-like transcripts of greater than 200 nucleotides (nt), with little or no protein-coding potential [13,14]. LncRNAs have been suggested to participate in transcription and post-transcription regulation as scaffolds, guides, decoys or repressors, activators, and

• For many plasma membrane receptors including GPCRs their den

  2021-12-23

  

  For many plasma membrane receptors including GPCRs, their density on the cell-surface is finely controlled by various transcriptional, post-transcriptional and post-translational mechanisms, and is often a determinant of overall receptor function in a cell. To date, the transcriptional regulation an

• There is a dual inducer of

  2021-12-23

  

  There is a dual inducer of both galanin and super-threshold pain. First, injury-induced pain may stimulate galanin secretion. After peripheral nerve injury, the galanin expression level was upregulated in dorsal root ganglion (DRG), dorsal horn and hypothalamic arcuate of rats [25], [28], [33]. The

• The chemical structure of BAs consists of a steroid

  2021-12-23

  

  The chemical structure of BAs consists of a steroid nucleus with an acidic side chain. They are amphipatic molecules characterized by a hydrophilic α-face and a hydrophobic β-face. The hydrophobic pocket of the FXR LBD interacts with BAs largely through the β-face. The α-face contains several hydrox

• Since our new compound Fex could be

  2021-12-22

  

  Since our new compound Fex-3 could be a new FXR ligand, we try to demonstrate that Fex-3 was an intestinal-restricted FXR agonist which only activated FXR in the intestine not in the liver or other organs. Initially, we investigated this in Caco-2 parecoxib with transwell experiments. From and , w

• Recent studies in our laboratory demonstrated that several h

  2021-12-22

  

  Recent studies in our laboratory demonstrated that several histamine H1 receptor antagonists induce apo A-I gene expression while histamine itself represses it [20]. In humans, there are three histamine receptor genes (H1, H2, and H3) that code for G-protein-coupled receptors (GPCR's) which bind his

• br Material and methods br Results br Discussion

  2021-12-22

  

  Material and methods Results Discussion Liver plays a key role in the metabolism and detoxification of DON (Peng et al., 2017). However, various DON investigations generated inconsistent results, with some showing hepatotoxicity of DON, while others not. For example, one report stated that

• Beside its role in NF B and IL

  2021-12-22

  

  Beside its role in NF-κB and IL-1β activation, the NRLP3 pathway is closely involved in another essential pathophysiologic mechanism such as the cellular calcium homeostasis. Full activation of the NRLP3 inflammasome requires decreased extracellular K concentrations resulting in decreased osmotic pr

• Gedunin Among prostaglandins PG PGD remained

  2021-12-22

  

  Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso

• In addition to their functional activation of

  2021-12-22

  

  In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic RF 9 to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner, whereas unlabeled

• The combination of niacin with

  2021-12-22

  

  The combination of niacin with a selective PGD2 receptor antagonist laropiprant, designed to circumvent the flushing side effect of niacin, has been evaluated in the HPS2-THRIVE study and showed no clinically meaningful benefit when administered in patients on top of statin therapy [41]. Our data su

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