• In recent years several DPP IV inhibitors have already been

  2022-02-08

  

  In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic NHS-12-Biotin with a unique xanthine scaffold developed through high-thro

• A linker length of and atoms was found to be

  2022-02-07

  

  A linker length of 4 and 5 atoms was found to be optimal ( and ) compared to the only weakly active compounds with longer linkers ( and ) or the inactive compounds with shorter linker chains (–). In a next step incorporation of hetero-atoms in the linker was explored (). An amide linker as in and d

• The calculations for the R substrate showed that like the

  2022-02-07

  

  The calculations for the R substrate showed that, like the S substrate, the coordination shell of the Zn phosphodiesterase is more symmetric than in the HIC-SG crystal structure. This symmetry indicates that the enzyme could use the same reaction mechanisms as for the S substrate, but with exchange

• br Conclusions The whole mRNA sequence of equine HRG

  2022-02-07

  

  Conclusions The whole mRNA sequence of equine HRG was identified. Consequently, we successfully generated recombinant equine HRG. By the Western blot procedure, blood HRG in horses was detected. Acknowledgments Introduction Alzheimer's disease (AD) is a chronic neurological disorder with c

• glutamate transporter Herein we report the discovery of AM

  2022-02-07

  

  Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to

• br Methods br Results and discussion br Conclusions A

  2022-02-07

  

  Methods Results and discussion Conclusions A third example of a hexokinase using polyphosphate exclusively as a phosphoryl donor has been identified, this time in mammalian tissues. This is the first polyphosphate utilizing enzyme activity demonstrated in mammalian GW3965 as far as we are

• br Conclusion In conclusion SHP was

  2022-02-07

  

  Conclusion In conclusion, SHP289-04 was demonstrated as a potent glucokinase activator. It could normalize the blood glucose level and lipid level in spontaneous type 2 diabetes model KKAy mice. At the same time, it ameliorated the function of islets and liver in KKAy mice. It had been proved to

• br Ghrelin and energy balance To characterize the physiologi

  2022-02-07

  

  Ghrelin and ubiquitin conjugating enzyme balance To characterize the physiological role of ghrelin in energy homeostasis, ghsr−/− and ghrelin−/− mice were generated [33], [36], [41], [47]. Although ghrelin regulates the amplitude of episodic GH release, ghsr−/− mice were not dwarfs, and in fact a

• 4-P-PDOT Almost all of the series and

  2022-02-05

  

  Almost all of the series and compounds exhibited higher activities compared with the compounds in the other series. In these series, the tetrazole group was directly linked to a nitrogen atom of the amide group at the C-28 position, and the C-3 hydroxy group was either unmodified, oxidized, esteri

• The concentration of rapamycin that gave half maximal induct

  2022-02-05

  

  The concentration of rapamycin that gave half-maximal induction of the expression of HO-1 and Prx-1 mRNA in normal hepatocytes was 0.05 μM, with maximal induction at about 0.1 μM rapamycin. While, at rapamycin concentrations higher than 0.1 μM, the degree of enzyme induction decreased, elevated expr

• br Materials and methods br Results br

  2022-02-04

  

  Materials and methods Results Discussion and conclusions Our data demonstrate that native and 2-OMe-LPC analogues are GPR119 ligands and activate insulin secretion from βTC-3 pancreatic cells. LPC 18:1 was the first proposed endogenous ligand for GPR119 [1], however natural LPC has limited

• To help resolve the question of simple binding versus

  2022-02-04

  

  To help resolve the question of simple binding versus transport, we reasoned that if quercetin is transported by GLUT1, we should be able to block its uptake by other GLUT1 inhibitors. We initially investigated the effects of two newly identified GLUT1 inhibitors, BAY-876 and WZB-117. WZB-117 was fi

• The main aim of our study was to identify

  2022-02-03

  

  The main aim of our study was to identify whether glucokinase and Irs2 were required for beta cell replication induced by short-term HF diet feeding. Glucokinase plays a critical role in regulating blood glucose levels by catalysing the rate-limiting biochemical reaction of glycolysis [26,27]. In pa

• Recently several dual GLP GIP receptor agonists have

  2022-02-03

  

  Recently, several dual GLP-1/GIP receptor agonists have been developed as a treatment of type II diabetes. These peptides can activate both the GLP-1 and the GIP receptor. Such dual receptor agonists are superior compared to single GLP-1 analogues such as liraglutide (Finan et al., 2013). Previously

• The effects of GHS R a blockade on

  2022-02-03

  

  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 consist

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