• GK allosteric activators validate the importance of GK from

  2021-09-13

  

  GK allosteric activators validate the importance of GK from a therapeutic perspective, but the nature of allosteric activation of GK remains unclear. The GK allosteric activator site, the pocket where GKAs bind, is ~20 Å remote from the active site (Fig. 1A). The allosteric site is the locus of many

• br Introduction The growth hormone secretagogue receptor GHS

  2021-09-13

  

  Introduction The growth hormone secretagogue receptor (GHSR) gene, which was first isolated from rats and humans (Kojima et al., 1999), comprises two exons and one intron in mammals and chicken. The pig GHSR is located on chromosome 13 (range 110,981,465–111,006,149 on Reference Sscrofa11.1). Alt

• It has also been demonstrated that

  2021-09-13

  

  It has also been demonstrated that PS1 is ubiquitinated by Caenorhabditis elegans SEL-10 [52], Fbw7 the mammalian homologue of SEL-10 [38], and more recently by tumour necrosis factor glycine transporter associated factor 6 (TRAF6), which facilitates Lysine-63 (K63)-linked polyubiquitination of PS1

• Galanin was shown to play an important

  2021-09-13

  

  Galanin was shown to play an important role in pain and pain processing [14] and the involvement of neuropeptides in the development of migraine is well established [[24], [25], [26]], however, so far it has not been examined whether systemic galanin levels correlate with migraine. Therefore, we use

• One effective approach to fine

  2021-09-13

  

  One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic nigericin synthesis scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as we

• We next determined the selectivity profile of the

  2021-09-13

  

  We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty n-acetyl-l-cysteine receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affinity

• cell tak Although exhibited high inhibitory activity was fou

  2021-09-13

  

  Although exhibited high inhibitory activity, was found to be metabolically unstable due to the hydrolysis of the phosphate group (data not shown), which prompted us to modify the phosphate moiety of . Comparison of the activities between three compounds bearing no or different spacer groups (, , a

• In tumor cells HK II induction is mediated

  2021-09-11

  

  In tumor cells HK-II induction is mediated by Akt/mTOR pathway [6], [11]. HK-II dynamically shuttles between the mitochondria and cytoplasm under different metabolic conditions. In cardiomyocytes, Akt enhances HK-II binding to mitochondria, setting the heart at a state resistant to ischemic injury [

• br Material and methods br Results br Discussion Organisms

  2021-09-11

  

  Material and methods Results Discussion Organisms have developed a variety of anti-glycation defense mechanisms. In Nuclear/Cytosol Fractionation Kit to the aldose-reductase-pathway or 2-oxoaldehyde dehydrogenase-pathway, the glyoxalase system is the only mechanism, which is not restricted

• Excessive extracellular glutamate can be removed from brain

  2021-09-11

  

  Excessive extracellular glutamate can be removed from droperidol synthesis interstitial fluids to the blood plasma for the maintenance of proper extracellular glutamate homeostasis in the mammalian central nervous system [[5], [6], [7]]. The glutamate concentration in the blood plasma increases in

• br Author contribution br Declaration of

  2021-09-11

  

  Author contribution Declaration of interest Acknowledgements This work was supported by National Natural Science Foundation of China (Grants 81473093) and State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM1601ZZ-02). Introduction Diabetes represents a majo

• The role of the cyclic AMP regulated exchange factor Epac

  2021-09-11

  

  The role of the cyclic AMP regulated exchange factor Epac1 is emerging in cancer (Almahariq et al., 2015, Banerjee and Cheng, 2015, Parnell et al., 2015, Parnell et al., 2015, Schmidt et al., 2013). Interestingly, in cancer cell migration, activation of Epac1 can be linked to activation of Rac. As s

• energy metabolism The gsnor ko plants contain elevated amoun

  2021-09-11

  

  The gsnor-ko plants contain elevated amount of low and high molecular weight S-nitrosothiols (SNO) indicating that GSNOR activity controls the level of both GSNO and indirectly protein-SNOs [13], [17], [18]. GSNOR deficiency has been shown to cause pleiotropic plant growth defects, impaired plant di

• In normal tissues the expression patterns

  2021-09-11

  

  In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet PD 0325901 and intestinal tract [7], [20]. It is considered that the distribution of the GPR1

• A number of synthetic GPR agonists have been

  2021-09-11

  

  A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,

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