• The G protein coupled receptor GPR also

  2022-03-04

  

  The G protein-coupled receptor, GPR40 (also called FFAR1) responds to medium and long chain unsaturated fatty acids, resulting in increase of insulin secretion during elevated glucose levels. The glucose dependency of insulin secretion makes this receptor a very good target for developing therapies

• Active compounds and were further

  2022-03-04

  

  Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of

• The subcellular redistribution of some metabolic enzymes is

  2022-03-04

  

  The subcellular redistribution of some metabolic enzymes is dynamic and responsive to metabolic conditions. In the absence of glucose, Glucokinase (GK) is bound to its regulatory protein in the nucleus of the hepatocyte and translocates to the cytoplasm when sugar levels increase [12]. Muscle glycog

• Apoptosis via Fas FasL system has been evidenced to

  2022-03-04

  

  Apoptosis via Fas/FasL system has been evidenced to play a role in the pathogenesis of many diseases [26], [27], [28], [29], [30], [31], [32], [33], [34]. Along with these, Fas/FasL system has an important role in progressive renal disease and organ rejection in renal, cardiac and liver transplanta

• Thus far it is reported that

  2022-03-03

  

  Thus far, it is reported that the histone methyltransferase activity of SUV39H1 is regulated through some posttranslational modifications. For example, deacetylation of SUV39H1 at Lys-266 by SIRT1 deacetylase increases SUV39H1 activity [31], and methylation of SUV39H1 at Lys-105 and Lys-123 by SET7

• br Histamine H R The cloning of the H

  2022-03-03

  

  Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other IT-901 receptor receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et al., 2009

• Recent studies in our laboratory demonstrated that several

  2022-03-03

  

  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

• Betahistine N methyl pyridyl ethylamine is a well known

  2022-03-03

  

  Betahistine (N-methyl-2-(2-pyridyl)ethylamine) is a well-known dual H1 Relevance agonist/H3 receptor antagonist with structural resemblance to histamine. Though it has been approved long before the discovery of H3R to treat disorders of vestibular function as Menières-Disease, the evidence for this

• br Conflict of interest statements br Acknowledgements br In

  2022-03-03

  

  Conflict of interest statements Acknowledgements Introduction Oral squamous cell carcinoma (OSCC) is the sixth most common cancer worldwide and is the major cause for cancer morbidity and mortality in developing countries. Age standardized incidence rate in India is 12.6 per 100 000 populat

• A general synthetic pathway to these tricyclic structures is

  2022-03-03

  

  A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methy

• GPR is a member of

  2022-03-03

  

  GPR119 is a member of the G protein-coupled receptor family, and is highly expressed in pancreatic β-cells and intestinal endocrine cells. It has been proposed that GPR119 agonists modulate glucose homeostasis by indirectly stimulating glucose-dependent insulin release through enhancing pancreatic c

• BCCA occlusion followed by reperfusion

  2022-03-03

  

  BCCA occlusion, followed by reperfusion injury, significantly increased the brain AT1 and AT2 receptor expression in mice. Reports have demonstrated elevation of AT1 receptor expression in the cerebral vx680 during ischemia [34,35]. The gene expression of brain AT2 receptor is increased in both in

• br Materials and methods br Results br Discussion To the

  2022-03-03

  

  Materials and methods Results Discussion To the best of our knowledge, the current study presented the first evidence that GPR40, also named FFAR1, played an essential role in bone formation and mediated Kartogenin induced osteogenic effect via Wnt/β-catenin signaling. We found that dose–r

• In this study we present the synthesis and structure

  2022-03-03

  

  In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g

• Injury to oligodendrocyte progenitors caused

  2022-03-03

  

  Injury to oligodendrocyte progenitors caused in part by glutamate contributes to the pathogenesis of myelination disturbances in PVL [5]. In the immature human brain, the susceptibility of developing oligodendrocytes to hypoxia-ischemia correlates with their expression of glutamate receptors of the

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