• Based on work from our labs with mGlu

  2022-07-16

  

  Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]

• A high throughput screening campaign of

  2022-07-16

  

  A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also co

• Abnormal expression and higher activity

  2022-07-16

  

  Abnormal expression and higher activity of GLO I have been detected more in various tumor rvx mg than in normal cell samples., , , , , , , Among cancer cell lines, lung carcinoma cells frequently showed higher GLO1 activity. Human NSCLC cell line NCI-H522 cells possess high activity and expression

• A number of experimental data declare a tight interdependenc

  2022-07-16

  

  A number of experimental data declare a tight interdependence between the pathological changes of glutamate transport in Gambogic Acid and consequent alterations in glutamate transport and activity/expression of glutamate metabolizing enzymes in platelets (Aliprandi et al., 2005, Behari and Shrivas

• Rifampicin that is methyl piperazinyl

  2022-07-16

  

  Rifampicin, that is 3-[[(4-methyl-1-piperazinyl) imino] methyl]-rifamycin (Fig. 1), is a semisynthetic antibiotic drug. It is one of the most potent and broad drug against bacterial pathogens and tuberculosis [9]. In recent years, rifampicin has also been reported to have inhibitory effects on Taq R

• In summary this study shows that compound d has strong

  2022-07-16

  

  In summary, this study shows that compound 4d has strong clinical potential as an efficient GLP-1/GCGR agonist exhibits weight-lowering, lipid-regulation and diabetes-protective effects and plays an important role in the prevention and therapy of diet induced obesity and dyslipidemia. The present st

• Murine models of sickle disease have been valuable tools

  2022-07-16

  

  Murine models of sickle disease have been valuable tools in the study of human SCD pathogenesis [15], [16], and will continue to be central to development of novel approaches to disease treatment. The SAD mouse model of sickle disease is particularly remarkable for its erythrocyte dehydration phenot

• br Gap junctions hemichannels and

  2022-07-16

  

  Gap junctions, hemichannels and connexins: Molecular characteristics and function Cell-to-cell communication is of extreme importance in tissue homeostasis, which is maintained by transmission of regulatory signals (Fig. 1). Intercellular communication via gap junctions (GJs) represents one of th

• br The glyoxalase system has

  2022-07-15

  

  The glyoxalase system has not yet been studied in E. histolytica or G. lamblia. Searches in the G. lamblia genome (GiardiaDB.org) revealed two genes encoding hydroxyacylglutathione hydrolases (Morrison et al., 2007), but no glyoxalase I gene was found. The genome of E. histolytica does not have a

• The effect of GCK NES mutations on enzyme kinetics

  2022-07-14

  

  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

• Rare mutations can impair the molecular function

  2022-07-14

  

  Rare mutations can impair the molecular function of GR and alter tissue sensitivity to GCs in humans, resulting in primary generalized GC resistance (PGGR) and hypersensitivity (PGGH) [14]. Familial and sporadic PGGR, or Chrousos Syndrome, is characterized by general and partial insensitivity of tis

• Fluorescein-12-dUTP The genes for the receptors for peptides

  2022-07-14

  

  The genes for the receptors for peptides similar to glucagon are dispersed on three human chromosomes, with two on chromosome 17 (GCGR and GLP2R) and one each on chromosomes 6 (GLP1R) and 19 (GIPR) (see Table S1). The exon–intron gene structures of these genes are similar, as are the genes for other

• br The interrelationship between obesity and galanin Numerou

  2022-07-14

  

  The interrelationship between obesity and galanin Numerous studies revealed that obesity and galanin may promote each other. On the one hand, galanin may increase the possibility of obesity of subjects via boosting their appetite and food intake. Acute injection with galanin or its agonist, galan

• Introduction Risk factors for colorectal cancer CRC

  2022-07-14

  

  Introduction Risk factors for colorectal cancer (CRC) include high-fat diets, sedentary lifestyles, obesity, diabetes, and elevated serum levels of toxic bile acids (BAs) (de Aguiar Vallim et al., 2013, Degirolamo et al., 2011, Downes and Liddle, 2008, Font-Burgada et al., 2016, Kuipers et al., 201

• FFAs are essential nutritional molecules that can

  2022-07-14

  

  FFAs are essential nutritional molecules that can also modulate numerous cellular functions. Fatty RF 9 receptor derivatives like prostaglandins, leukotrienes lysophosphatidic acid, spinhgosine-1-phosphate and others are well documented to carry out signal transduction via G-protein coupled recepto

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